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

Abacavir [136470-78-5]

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Referencia HY-17423-10mg

embalaje : 10mg

Marca : MedChemExpress

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Descripciòn

Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity^[1]^[2]^[3].

Cellular Effect

Cell Line	Type	Value	Description	References
C3H/3T3	CC₅₀	>20 μM Compound: 1	Cytostatic concentration required to inhibit C3H/3T3 cell proliferation Cytostatic concentration required to inhibit C3H/3T3 cell proliferation	[PMID: 15887959]
C3H/3T3	EC₅₀	8.8 μM Compound: 1	Effective concentration against murine moloney sarcoma virus in C3H/3T3 cells Effective concentration against murine moloney sarcoma virus in C3H/3T3 cells	[PMID: 15887959]
CCRF-CEM	CC₅₀	78 μM Compound: 1	Cytostatic concentration required to inhibit CEM cell proliferation Cytostatic concentration required to inhibit CEM cell proliferation	[PMID: 15887959]
CCRF-CEM	EC₅₀	1.9 μM Compound: 1	Effective concentration against human immunodeficiency virus type 1 in CEM cells Effective concentration against human immunodeficiency virus type 1 in CEM cells	[PMID: 15887959]
CCRF-CEM	EC₅₀	3 μM Compound: 1	Effective concentration against human immunodeficiency virus type 2 (ROD) in CEM cells Effective concentration against human immunodeficiency virus type 2 (ROD) in CEM cells	[PMID: 15887959]
CCRF-CEM	EC₅₀	3 μM Compound: 1	Effective concentration against human immunodeficiency virus type 2 in CEM cells Effective concentration against human immunodeficiency virus type 2 in CEM cells	[PMID: 15887959]
CCRF-CEM	CC₅₀	83 μM Compound: Abacavir	Cytotoxicity against CEM cell line Cytotoxicity against CEM cell line	[PMID: 16458506]
CCRF-CEM	EC₅₀	1.6 μM Compound: Abacavir	Antiviral activity against HIV1 replication in CEM cell line Antiviral activity against HIV1 replication in CEM cell line	[PMID: 16458506]
CCRF-CEM	CC₅₀	>250 μM Compound: 11, ABC	Cytotoxicity against human CEM cells Cytotoxicity against human CEM cells	[PMID: 24177359]
CCRF-CEM	EC₅₀	18 μM Compound: 11, ABC	Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis	[PMID: 24177359]
CCRF-CEM	EC₅₀	23 μM Compound: 11, ABC	Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis	[PMID: 24177359]
CCRF-CEM	IC₅₀	>250 μM Compound: 11, ABC	Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
HEL	CC₅₀	200 μM Compound: 1	Cytostatic concentration required to inhibit HEL cell proliferation Cytostatic concentration required to inhibit HEL cell proliferation	[PMID: 15887959]
HeLa	IC₅₀	170 μM Compound: 11, ABC	Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
HepG2	CC₅₀	110 μM Compound: 1	Cytostatic concentration required to inhibit Hep G2 cell proliferation Cytostatic concentration required to inhibit Hep G2 cell proliferation	[PMID: 15887959]
HepG2 2.2.15	EC₅₀	5.6 μM Compound: 1	Effective concentration against HBV in Hep G2.2.15 cells Effective concentration against HBV in Hep G2.2.15 cells	[PMID: 15887959]
HepG2 2.2.15	EC₅₀	5.6 μM Compound: 1	Effective concentration againstHBV in Hep G2.2.15 cells Effective concentration againstHBV in Hep G2.2.15 cells	[PMID: 15887959]
L1210	IC₅₀	>250 μM Compound: 11, ABC	Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis	[PMID: 24177359]
MT2	CC₅₀	190 μM Compound: Abacavir	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 18029175]
MT2	CC₅₀	190 μM Compound: 5, abacavir	Cytotoxicity against human MT2 cells after 5 days Cytotoxicity against human MT2 cells after 5 days	[PMID: 19179082]
MT2	EC₅₀	0.32 μM Compound: 5, abacavir	Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay	[PMID: 19179082]
MT4	EC₅₀	7.3 μM Compound: 1	Effective concentration against human immunodeficiency virus type 2 in MT-4 cells Effective concentration against human immunodeficiency virus type 2 in MT-4 cells	[PMID: 15887959]
PBL	EC₅₀	0.2 μM Compound: 1	Effective concentration against human immunodeficiency virus type 1 in PBL cells Effective concentration against human immunodeficiency virus type 1 in PBL cells	[PMID: 15887959]

In Vitro

Abacavir (15 and 150 μM, 0-120 h) inhibits cell growth, affects cell cycle progression, induces senescence and modulates LINE-1 mRNA expression in prostate cancer cell lines^[1].
Abacavir (15 and 150 μM, 18 h) significantly reduces cell migration and inhibits cell invasion^[1].
Abacavir induces fat apoptosis^[4].

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

Cell Proliferation Assay^[1]

Cell Line:	PC3, LNCaP and WI-38
Concentration:	15 and 150 μM
Incubation Time:	0, 24, 48, 72 and 96 h
Result:	Showed a dose-dependent growth inhibition on PC3 and LNCaP.

Cell Cycle Analysis^[1]

Cell Line:	PC3 and LNCaP
Concentration:	150 μM
Incubation Time:	0, 18, 24, 48, 72, 96 and 120 h
Result:	Caused a very high accumulation of cells in S phase in PC3 and LNCaP cells, and G2/M phase increment was observed in PC3 cells.

Cell Migration Assay ^[1]

Cell Line:	PC3 and LNCaP
Concentration:	15 and 150 μM
Incubation Time:	18 h
Result:	Significantly reduced cell migration.

Cell Invasion Assay^[1]

Cell Line:	PC3 and LNCaP
Concentration:	15 and 150 μM
Incubation Time:	18 h
Result:	Significantly inhibited cell invision.

In Vivo

Abacavir (100 and 200 mg/kg, p.o.; 4 h) dose-dependently promoted thrombus formation^[2].
Abacavir (50 mg/kg/d; i.p.; 14 d) with 0.1 mg/kg/d Decitabine (HY-A0004) enhances survival of high-risk medulloblastoma-bearing mice^[3].

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

Animal Model:	Male mice (9-weeks old, 22-30 g) - wild-type (WT) C57BL/6 or homozygous knockout (P2rx7 KO, B6.129P2-P2rx7^tm1Gab/J)^[2]
Dosage:	2.5, 5 and 7.5 μg/mL, 100 μL or 100 and 200 mg/kg
Administration:	Intrascrotal or oral administration for 4 h
Result:	Dose-dependently promoted thrombus formation.

Animal Model:	NSG^TM mice, patient-derived xenograft (PDX) cells of non-WNT/non-SHH, Group 3 and of SHH/ TP53-mutated medulloblastoma^[3]
Dosage:	50 mg/kg/d with 0.1 mg/kg/d Decitabine
Administration:	Intraperitoneal injection, daily for 14 days
Result:	Inhibited tumor growth and enhanced mouse survival.

Ensayo clínico

Peso molecular

286.34

Fòrmula

C₁₄H₁₈N₆O

No. CAS

136470-78-5

Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(NC2CC2)=C3N=CN([C@H]4C=C[C@@H](CO)C4)C3=N1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (349.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (6.98 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4924 mL	17.4618 mL	34.9235 mL
5 mM	0.6985 mL	3.4924 mL	6.9847 mL
10 mM	0.3492 mL	1.7462 mL	3.4924 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: ≥ 2.5 mg/mL (8.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (8.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (8.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: PBS
Solubility: 3.33 mg/mL (11.63 mM); Clear solution; Need ultrasonic and warming

Pureza y Documentación

Purity: 99.88%

Ficha de datos (289 KB) SDS (419 KB)

COA (248 KB) HNMR (163 KB) RP-HPLC (236 KB) MS (205 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Carlini F, et al. The reverse transcription inhibitor abacavir shows anticancer activity in prostate cancer cell lines. PLoS One. 2010 Dec 3;5(12):e14221. [Content Brief]

[2]. Collado-Diaz V, et al. Abacavir Induces Arterial Thrombosis in a Murine Model. J Infect Dis. 2018 Jun 20;218(2):228-233. [Content Brief]

[3]. Gringmuth M, et al. Enhanced Survival of High-Risk Medulloblastoma-Bearing Mice after Multimodal Treatment with Radiotherapy, Decitabine, and Abacavir. Int J Mol Sci. 2022 Mar 30;23(7):3815. [Content Brief]

[4]. McComsey GA, et al. Improvements in lipoatrophy, mitochondrial DNA levels and fat apoptosis after replacing stavudine with abacavir or zidovudine. AIDS. 2005 Jan 3;19(1):15-23. [Content Brief]

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Abacavir [136470-78-5]

Referencia HY-17423-10mg

Marca : MedChemExpress

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