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

Selumetinib [606143-52-6]

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Referencia HY-50706-50mg

embalaje : 50mg

Marca : MedChemExpress

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Descripciòn

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib can penetrate the blood brain barrier (BBB)^[1]^[2]^[3]^[4].

IC₅₀ & Target^[3]^[4]

MEK

12 nM (IC₅₀)

MEK1

14 nM (IC₅₀)

MEK2

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	31 nM Compound: AZD6244	Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay	[PMID: 23474388]
A549	CC₅₀	> 100 μM Compound: 39; AZD6244	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
A549	IC₅₀	1750 nM Compound: AZD6244	Antiproliferative activity against human A549 cells Antiproliferative activity against human A549 cells	[PMID: 23474388]
A549	IC₅₀	1750 nM Compound: AZD6244	Antiproliferative activity against human A549 cells harboring K-Ras mutation Antiproliferative activity against human A549 cells harboring K-Ras mutation	[PMID: 26611920]
A549	IC₅₀	> 100 μM Compound: AZD6244	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: 30777660]
ASPC1	IC₅₀	64.2 nM Compound: AZD6244; AZD	Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
BaF3	IC₅₀	100 nM Compound: AZD6244; AZD	Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
BaF3	IC₅₀	> 1 x 10^-4n M Compound: AZD6244; AZD	Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay	[PMID: 28038940]
COLO 205	IC₅₀	59 nM Compound: AZD6244	Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay	[PMID: 29317148]
COLO 205	IC₅₀	69 nM Compound: AZD6244	Antiproliferative activity against human COLO205 cells harboring BRAF mutation Antiproliferative activity against human COLO205 cells harboring BRAF mutation	[PMID: 26611920]
DLD-1	IC₅₀	1.25 μM Compound: 41	Anticancer activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay Anticancer activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay	[PMID: 33445154]
HCT-116	IC₅₀	0.95 μM Compound: 41	Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay	[PMID: 33445154]
HCT-116	IC₅₀	3000 nM Compound: AZD6244	Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation	[PMID: 26611920]
HCT-116	IC₅₀	3100 nM Compound: AZD6244	Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant	[PMID: 23474388]
HepG2	IC₅₀	32 nM Compound: AZD6244	Antiproliferative activity against human HepG2 cells harboring N-Ras mutation Antiproliferative activity against human HepG2 cells harboring N-Ras mutation	[PMID: 26611920]
LoVo	IC₅₀	2830 nM Compound: AZD6244	Antiproliferative activity against human LoVo cells Antiproliferative activity against human LoVo cells	[PMID: 23474388]
MCF7	IC₅₀	> 10000 nM Compound: AZD6244	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 26611920]
MIA PaCa-2	IC₅₀	142 nM Compound: AZD6244	Antiproliferative activity against human MIAPaCa2 cells Antiproliferative activity against human MIAPaCa2 cells	[PMID: 23474388]
Malme-3M	IC₅₀	59 nM Compound: 60	Antiproliferative activity against human Malme-3M cells assessed as inhibition of cell growth Antiproliferative activity against human Malme-3M cells assessed as inhibition of cell growth	[PMID: 36155354]
PANC-1	IC₅₀	> 1 x 10^-4n M Compound: AZD6244; AZD	Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
SK-CO-1	IC₅₀	117 nM Compound: AZD6244; AZD	Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
SW-620	IC₅₀	15 nM Compound: AZD6244; AZD	Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
SW480	IC₅₀	0.422 μM Compound: AZD6244	Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay	[PMID: 27448918]

In Vitro

Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells^[1].
Selumetinib (AZD6244) (1μM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells^[2].
Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line^[3].

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

Solvente y solubilidad

In Vitro:

DMSO : 20.83 mg/mL (45.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1849 mL	10.9247 mL	21.8493 mL
5 mM	0.4370 mL	2.1849 mL	4.3699 mL
10 mM	0.2185 mL	1.0925 mL	2.1849 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (21.85 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Purity: 99.72%

Ficha de datos (283 KB) SDS (396 KB)

COA (252 KB) HNMR (228 KB) LCMS (162 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Huynh H, et al, Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Therapy, 2007, 6 (1), 138-146 [Content Brief]

[2]. Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994. [Content Brief]

[3]. Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res, 2007, 13 (5), 1576-1583. [Content Brief]

[4]. Sebolt-Leopold JS, et al. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer. 2004 Dec;4(12):937-47. [Content Brief]

[5]. Sara H Osum, et al. Selumetinib normalizes Ras/MAPK signaling in clinically relevant neurofibromatosis type 1 minipig tissues in vivo. Neurooncol Adv. 2021 Feb 10;3(1):vdab020. [Content Brief]

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Selumetinib [606143-52-6]

Referencia HY-50706-50mg

Marca : MedChemExpress

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