Reactivos e instrumentos para inmunología, biología celular y biología molecular.

Tanespimycin [75747-14-7]

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Referencia HY-10211-1mL

embalaje : 10mM/1mL

Marca : MedChemExpress

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Descripciòn

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90^[1]^[5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression^[3].

IC₅₀ & Target^[5]

HSP90

5 nM (IC₅₀)

Autophagy

Mitophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1287 nM Compound: 2, 17-AAG	Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
A-375	IC₅₀	32 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening	[PMID: 19552433]
A-375	IC₅₀	4 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening	[PMID: 19552433]
A-431	IC₅₀	0.07 μM Compound: 17-AAG	Antiproliferative activity against human A431 cells after 72 hrs Antiproliferative activity against human A431 cells after 72 hrs	[PMID: 20655237]
A-431	IC₅₀	0.069 μM Compound: 17-AAG	Cytotoxicity against human A431 cells after 72 hrs Cytotoxicity against human A431 cells after 72 hrs	[PMID: 22538015]
A-431	IC₅₀	89 nM Compound: 17-Aag	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 25277067]
A549	IC₅₀	81 nM Compound: 17-Aag	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25277067]
A549	IC₅₀	0.286 μM Compound: 2; 17-AAG	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 28073608]
A549	GI₅₀	0.0075 μM Compound: III; 17AAG	Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
A549	IC₅₀	>10 μM Compound: 17-AAG	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
A549	IC₅₀	>10 μM Compound: 4; 17-AAG	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
A549	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
AU565	IC₅₀	0.003 μM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening	[PMID: 19552433]
AU565	IC₅₀	8 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening	[PMID: 19552433]
B16-F10	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against mouse B16F10 Antiproliferative activity against mouse B16F10	[PMID: 21972823]
BGC-823	IC₅₀	847 nM Compound: 17-Aag	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 25277067]
BT-474	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human BT474 cells by MTS assay Antiproliferative activity against human BT474 cells by MTS assay	[PMID: 17488003]
BT-474	GI₅₀	5 nM Compound: 3, 17-AAG	Growth inhibition of human BT474 cells assessed as ATP level after 4 days Growth inhibition of human BT474 cells assessed as ATP level after 4 days	[PMID: 19410458]
CCRF-CEM	IC₅₀	0.1 μM Compound: 17-AAG	Antiproliferative activity against human CEM Antiproliferative activity against human CEM	[PMID: 21972823]
CNE-2	IC₅₀	3.03 μM Compound: 17-AAG	Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
CNE2Z	IC₅₀	8.41 μM Compound: 17-AAG	Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
DU-145	IC₅₀	68.3 μM Compound: 17-AAG	Cytotoxicity against DU145 cells after 72 hrs Cytotoxicity against DU145 cells after 72 hrs	[PMID: 17181154]
DU-145	IC₅₀	0.282 μM Compound: 2; 17-AAG	Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay	[PMID: 28073608]
ECa-109 cell line	IC₅₀	1.1 μM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay	[PMID: 23621840]
GES1	CC₅₀	7.94 μM Compound: 4; 17-AAG	Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
HCC827	GI₅₀	56 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days	[PMID: 19410458]
HCT-116	GI₅₀	0.021 μM Compound: 1b 17AAG	Inhibition of HCT116 human colon cancer cell proliferation Inhibition of HCT116 human colon cancer cell proliferation	[PMID: 15955698]
HCT-116	GI₅₀	0.16 μM Compound: 17-AAG	Inhibitory concentration against cell proliferation of human HCT116 cell Inhibitory concentration against cell proliferation of human HCT116 cell	[PMID: 15974572]
HCT-116	GI₅₀	0.16 μM Compound: 17-AAG	Inhibition of cell proliferation in HCT116 human colon cancer cell line Inhibition of cell proliferation in HCT116 human colon cancer cell line	[PMID: 16202589]
HCT-116	IC₅₀	0.17 μM Compound: 17-AAG	Antiproliferative activity against HCT116 cell line Antiproliferative activity against HCT116 cell line	[PMID: 16480864]
HCT-116	GI₅₀	0.16 μM Compound: 1b, 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by SRB assay Growth inhibition of human HCT116 cells after 24 hrs by SRB assay	[PMID: 18020435]
HCT-116	IC₅₀	202 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human HCT116 cells after 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs	[PMID: 19231864]
HCT-116	IC₅₀	56.5 nM Compound: 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay	[PMID: 20014866]
HCT-116	IC₅₀	0.145 μM Compound: 17-AAG	Antiproliferative activity against human HCT116 Antiproliferative activity against human HCT116	[PMID: 21972823]
HCT-116	GI₅₀	0.34 μM Compound: III; 17AAG	Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
HCT-116	GI₅₀	0.34 μM Compound: 1; 17-AAG	Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HCT-15	IC₅₀	1487 nM Compound: 2, 17-AAG	Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HCT-15	IC₅₀	0.41 μM Compound: 17-AAG	Antiproliferative activity against human HCT15 Antiproliferative activity against human HCT15	[PMID: 21972823]
HeLa	IC₅₀	108.2 μM Compound: 17-AAG	Cytotoxicity against HeLa cells after 72 hrs Cytotoxicity against HeLa cells after 72 hrs	[PMID: 17181154]
HeLa	IC₅₀	128 nM Compound: 17-Aag	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25277067]
HeLa	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay	[PMID: 27266997]
HeLa	IC₅₀	>1000 μM Compound: III; 17AAG	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay	[PMID: 31655430]
HeLa	IC₅₀	19.4 μM Compound: 17-AAG	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
Hep 3B2	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HepG2	IC₅₀	91 nM Compound: 17-Aag	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 25277067]
HepG2	IC₅₀	0.32 μM Compound: 17-AAG	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
HepG2	IC₅₀	0.33 μM Compound: 4; 17-AAG	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
HepG2	IC₅₀	8 μM Compound: 17-AAG	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
HL-60	IC₅₀	0.06 μM Compound: 17-AAG	Antiproliferative activity against human HL60 Antiproliferative activity against human HL60	[PMID: 21972823]
HT-29	IC₅₀	0.002 μM Compound: 17-AAG	Antiproliferative activity against human HT29 cells Antiproliferative activity against human HT29 cells	[PMID: 17488003]
HT-29	IC₅₀	0.1 nM Compound: 2, 17-AAG	Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HT-29	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human HT-29 Antiproliferative activity against human HT-29	[PMID: 21972823]
HUVEC	IC₅₀	282 nM Compound: 17-Aag	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay Cytotoxicity against HUVEC cells after 72 hrs by MTT assay	[PMID: 25277067]
HUVEC	GI₅₀	<0.1 μM Compound: 1; 17-AAG	Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
K562	GI₅₀	48 nM Compound: 3, 17-AAG	Growth inhibition of human K562 cells assessed as ATP level after 4 days Growth inhibition of human K562 cells assessed as ATP level after 4 days	[PMID: 19410458]
K562	IC₅₀	126 nM Compound: 2, 17-AAG	Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
K562	IC₅₀	0.15 μM Compound: 1, 17-AAG	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay	[PMID: 24565573]
L02	IC₅₀	99 nM Compound: 17-Aag	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25277067]
L02	CC₅₀	11.65 μM Compound: 4; 17-AAG	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
LNCaP	IC₅₀	82 nM Compound: 2, 17-AAG	Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
LNCaP	IC₅₀	0.16 μM Compound: 17-AAG	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 25105924]
LoVo	IC₅₀	0.26 μM Compound: 4; 17-AAG	Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
MCF7	IC₅₀	>500 μM Compound: 17AAG	Inhibition of Phoshoinositol 3 kinase from MCF-7 breast cancer cells Inhibition of Phoshoinositol 3 kinase from MCF-7 breast cancer cells	[PMID: 11294389]
MCF7	IC₅₀	0.007 μM Compound: 17-AAG	Inhibition of human recombinant HSP90 in MCF7 cells assessed as Her2 degradation Inhibition of human recombinant HSP90 in MCF7 cells assessed as Her2 degradation	[PMID: 17488003]
MCF7	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells by MTS assay Antiproliferative activity against human MCF7 cells by MTS assay	[PMID: 17488003]
MCF7	IC₅₀	0.02 μM Compound: 17-AAG	Binding affinity to human recombinant HSP90 in MCF7 cell lysates assessed as inhibition of biotinylated-geldanamycin binding Binding affinity to human recombinant HSP90 in MCF7 cell lysates assessed as inhibition of biotinylated-geldanamycin binding	[PMID: 17488003]
MCF7	IC₅₀	50 μM Compound: 17-AAG	Selectivity for HSP90 in MCF7 cells over HSP90 in NDF cells Selectivity for HSP90 in MCF7 cells over HSP90 in NDF cells	[PMID: 17488003]
MCF7	IC₅₀	15 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation	[PMID: 19017562]
MCF7	IC₅₀	58 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs	[PMID: 19231864]
MCF7	IC₅₀	662 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
MCF7	IC₅₀	0.3 nM Compound: 2, 17-AAG	Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MCF7	IC₅₀	12 nM Compound: 3, 17-AAG, KOS953, CNF-1010	Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells	[PMID: 20055425]
MCF7	IC₅₀	0.09 μM Compound: 1b, 17-AAG	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 21920765]
MCF7	EC₅₀	12 nM Compound: 1, 17-AAG, tanespimycin	Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2 Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2	[PMID: 22938030]
MCF7	IC₅₀	0.029 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MCF7	IC₅₀	5 nM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay	[PMID: 27153346]
MCF7	IC₅₀	0.192 μM Compound: 2; 17-AAG	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 28073608]
MCF7	IC₅₀	0.005 μM Compound: 49; 17-AAG	Antitumor activity against human MCF7 cells assessed as cell growth inhibition Antitumor activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 36858050]
MCF7	IC₅₀	58 nM Compound: 2a; 17-AAG	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 39361055]
MDA-MB-231	IC₅₀	194 nM Compound: 2, 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-AAG	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25105924]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-Aag	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25277067]
MDA-MB-231	IC₅₀	0.52 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 27266997]
MDA-MB-231	IC₅₀	1.79 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
MDA-MB-231	GI₅₀	0.27 μM Compound: 1; 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
MDA-MB-468	IC₅₀	1500 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs	[PMID: 19231864]
MDA-MB-468	GI₅₀	780 nM Compound: 3, 17-AAG	Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days	[PMID: 19410458]
MDA-MB-468	IC₅₀	1.57 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MRC5	CC₅₀	14.24 μM Compound: 4; 17-AAG	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
MV4-11	GI₅₀	11 nM Compound: 3, 17-AAG	Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days	[PMID: 19410458]
MX1	IC₅₀	0.045 μM Compound: 17-AAG	Antiproliferative activity against human MX1 Antiproliferative activity against human MX1	[PMID: 21972823]
NCI-H1299	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay	[PMID: 28426997]
NCI-H1975	GI₅₀	35 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCI-H1975	GI₅₀	0.16 μM Compound: III; 17AAG	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
NCI-H460	IC₅₀	255 nM Compound: 2, 17-AAG	Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
NCI-H460	IC₅₀	0.03 μM Compound: 17-AAG	Antiproliferative activity against human NCI-H460 Antiproliferative activity against human NCI-H460	[PMID: 21972823]
NCI-H460	IC₅₀	0.01 μM Compound: 17-AAG	Cytotoxicity against human NCI-H460 cells after 72 hrs Cytotoxicity against human NCI-H460 cells after 72 hrs	[PMID: 22538015]
NCI-H596	IC₅₀	1600 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs	[PMID: 19231864]
NCI-N87	GI₅₀	1 nM Compound: 3, 17-AAG	Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCM460	CC₅₀	14.21 μM Compound: 4; 17-AAG	Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
OVCAR-3	IC₅₀	0.48 μM Compound: 4; 17-AAG	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PANC-1	IC₅₀	3.21 μM Compound: 4; 17-AAG	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PC-3	IC₅₀	9 nM Compound: 2, 17-AAG	Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
PC-3	IC₅₀	0.13 μM Compound: 17-AAG	Antiproliferative activity against human PC3 Antiproliferative activity against human PC3	[PMID: 21972823]
PC-3	IC₅₀	0.062 μM Compound: 17-AAG	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
RPTEC	IC₅₀	0.1 μM Compound: 17-AAG	Antiproliferative activity against human RPTEC Antiproliferative activity against human RPTEC	[PMID: 17488003]
RPTEC	IC₅₀	10 μM Compound: 17-AAG	Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for MCF7 cells Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for MCF7 cells	[PMID: 17488003]
RPTEC	IC₅₀	50 μM Compound: 17-AAG	Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for HT29 cells Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for HT29 cells	[PMID: 17488003]
SGC-7901	IC₅₀	>10 μM Compound: 4; 17-AAG	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
SK-BR-3	IC₅₀	27 nM Compound: 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay	[PMID: 15844961]
SK-BR-3	EC₅₀	22 nM Compound: 1b, 17-AAG	Upregulation of Hsp70 in SKBR3 cells Upregulation of Hsp70 in SKBR3 cells	[PMID: 16854066]
SK-BR-3	EC₅₀	35 nM Compound: 1b, 17-AAG	Degradation of Her2 in SKBR3 cells Degradation of Her2 in SKBR3 cells	[PMID: 16854066]
SK-BR-3	GI₅₀	17 nM Compound: 1b, 17-AAG	Inhibition of human SKBR3 cell growth Inhibition of human SKBR3 cell growth	[PMID: 16854066]
SK-BR-3	IC₅₀	31 nM Compound: 2, 17-AAG	Inhibition of Her2 in human SKBR3 cells Inhibition of Her2 in human SKBR3 cells	[PMID: 19017562]
SK-BR-3	IC₅₀	33 nM Compound: 2, 17-AAG	Binding affinity to Hsp90 in human SKBR3 cells Binding affinity to Hsp90 in human SKBR3 cells	[PMID: 19017562]
SK-BR-3	IC₅₀	410 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
SK-BR-3	IC₅₀	44 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs	[PMID: 19231864]
SK-BR-3	IC₅₀	33 nM Compound: 1b, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
SK-BR-3	EC₅₀	<0.1 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis	[PMID: 21106457]
SK-BR-3	EC₅₀	0.025 μM Compound: 1, 17-AAG	Cytotoxicity against human SKBR3 cells Cytotoxicity against human SKBR3 cells	[PMID: 21106457]
SK-BR-3	EC₅₀	0.06 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis	[PMID: 21106457]
SK-BR-3	IC₅₀	0.025 μM Compound: 17-AAG	Antiproliferative activity against human SKBR3 Antiproliferative activity against human SKBR3	[PMID: 21972823]
SK-BR-3	IC₅₀	0.038 μM Compound: 17-AAG	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-BR-3	IC₅₀	0.004 μM Compound: 49; 17-AAG	Antitumor activity against human SK-BR-3 cells assessed as cell growth inhibition Antitumor activity against human SK-BR-3 cells assessed as cell growth inhibition	[PMID: 36858050]
SK-BR-3	IC₅₀	31 nM Compound: 1b5	Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose. Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose.	[PMID: 7562911]
SK-BR-3	IC₅₀	31 nM Compound: 1c	In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells	[PMID: 7562912]
SK-MEL-5	IC₅₀	134 nM Compound: 2, 17-AAG	Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SK-OV-3	EC₅₀	19 nM Compound: 1b, 17-AAG	Degradation of Her2 in SKOV3 cells Degradation of Her2 in SKOV3 cells	[PMID: 16854066]
SK-OV-3	GI₅₀	15 nM Compound: 1b, 17-AAG	Inhibition of human SKOV3 cell growth Inhibition of human SKOV3 cell growth	[PMID: 16854066]
SK-OV-3	IC₅₀	240 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKOV3 cells after 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs	[PMID: 19231864]
SK-OV-3	IC₅₀	0.22 μM Compound: 17-AAG	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-OV-3	IC₅₀	240 nM Compound: 2a; 17-AAG	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 39361055]
SMMC-7721	IC₅₀	0.19 μM Compound: 17-AAG	Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	572 nM Compound: 17-Aag	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 25277067]
SW480	IC₅₀	0.28 μM Compound: 17-AAG	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW-620	IC₅₀	328 nM Compound: 2, 17-AAG	Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
U-87MG ATCC	IC₅₀	>10 μM Compound: 17-AAG	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]

In Vitro

Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC₅₀s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)^[1].
Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells^[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (85.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7074 mL	8.5369 mL	17.0739 mL
5 mM	0.3415 mL	1.7074 mL	3.4148 mL
10 mM	0.1707 mL	0.8537 mL	1.7074 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.62 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.07 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (8.54 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Purity: 99.01%

Ficha de datos (282 KB) SDS (393 KB)

COA (251 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993. [Content Brief]

[2]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163 [Content Brief]

[3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7. [Content Brief]

[4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29. [Content Brief]

[5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. [Content Brief]

[6]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58. [Content Brief]

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Referencia

Descripción

Cond.

Precio Sin IVA

T6290-1ml

Tanespimycin [75747-14-7]

1mLx10mM(inDMSO)

T3S0209-1ml

Vincristine [57-22-7]

1mLx10mM(inDMSO)

Tanespimycin [75747-14-7]

Referencia HY-10211-1mL

Marca : MedChemExpress

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