Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Venetoclax [1257044-40-8]

Imprimer

Référence HY-15531-10mg

Conditionnement : 10mg

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Description

Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy^[1]^[2]^[3].

IC₅₀ & Target^[1]

Bcl-2

0.01 nM (Ki)

Bcl-xL

48 nM (Ki)

Bcl-W

245 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
Cancer cell lines	GI₅₀	2.6 μM Compound: ABT-199	Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	2.7 μM Compound: ABT-199	Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	2.77 μM Compound: ABT-199	Cytotoxicity against human breast cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human breast cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	2.85 μM Compound: ABT-199	Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	3.33 μM Compound: ABT-199	Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	3.35 μM Compound: ABT-199	Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
Cancer cell lines	GI₅₀	3.51 μM Compound: ABT-199	Cytotoxicity against human prostate cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human prostate cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
HEK-293T	IC₅₀	> 20 μM Compound: ABT-199	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HeLa	IC₅₀	> 20 μM Compound: ABT-199	Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HL-60	IC₅₀	0.077 μM Compound: ABT-199	Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HL-60	EC₅₀	8.1 μM Compound: ABT-199	Induction of apoptosis in human HL-60 cells measured after 48 hrs by FITC-Annexin V/PS staining based Induction of apoptosis in human HL-60 cells measured after 48 hrs by FITC-Annexin V/PS staining based	[PMID: 33197310]
K562	EC₅₀	2.1 μM Compound: ABT199	Cytotoxicity against human K562 cells assessed as cell survival measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell survival measured after 72 hrs by MTT assay	[PMID: 34216984]
KG-1	EC₅₀	0.85 μM Compound: ABT-199	Induction of apoptosis in human KG-1 cells measured after 48 hrs by FITC-Annexin V/PS staining based Induction of apoptosis in human KG-1 cells measured after 48 hrs by FITC-Annexin V/PS staining based	[PMID: 33197310]
Leukemia cell	GI₅₀	2.11 μM Compound: ABT-199	Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
MCF7	EC₅₀	1.35 μM Compound: ABT-199	Induction of apoptosis in human MCF7 cells measured after 48 hrs by FITC-Annexin V/PS staining based Induction of apoptosis in human MCF7 cells measured after 48 hrs by FITC-Annexin V/PS staining based	[PMID: 33197310]
Melanoma cell	GI₅₀	1.75 μM Compound: ABT-199	Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 27994761]
OCI-AML-3	EC₅₀	6.8 μM Compound: ABT-199	Induction of apoptosis in human OCI-AML-3 cells measured after 48 hrs by FITC-Annexin V/PS staining based Induction of apoptosis in human OCI-AML-3 cells measured after 48 hrs by FITC-Annexin V/PS staining based	[PMID: 33197310]
RPMI-8226	IC₅₀	2.7 μM Compound: ABT-199	Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 30594434]
RS4-11	IC₅₀	0.0043 μM Compound: ABT-199	Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
RS4-11	IC₅₀	0.006 μM Compound: ABT-199; 1	Antiproliferative activity against human RS4:11 cells after 72 hrs by MTS assay Antiproliferative activity against human RS4:11 cells after 72 hrs by MTS assay	[PMID: 30278333]
RS4-11	IC₅₀	0.33 μM Compound: ABT-199	Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29453135]
RS4-11	IC₅₀	1.8 nM Compound: 6; ABT-199	Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34536651]
Toledo	IC₅₀	0.011 μM Compound: ABT-199; 1	Antiproliferative activity against human Toledo cells after 72 hrs by MTS assay Antiproliferative activity against human Toledo cells after 72 hrs by MTS assay	[PMID: 30278333]
U-266	IC₅₀	94 μM Compound: ABT-199	Growth inhibition of human U266 cells after 72 hrs by MTT assay Growth inhibition of human U266 cells after 72 hrs by MTT assay	[PMID: 30594434]

In Vitro

Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC₅₀=4 nM), Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC₅₀=261 nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC₅₀=3 nM) but is much less effective against BCL-XL-BCL-XS (EC₅₀=2.2 μM) or MCL-1-NOXA complexes^[1].

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

Solvant et solubilité

In Vitro:

DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1515 mL	5.7575 mL	11.5149 mL
5 mM	0.2303 mL	1.1515 mL	2.3030 mL
10 mM	0.1151 mL	0.5757 mL	1.1515 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.

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% Ethanol 60% Phosal 50 PG 30% PEG400
Solubility: 20 mg/mL (23.03 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 5 mg/mL (5.76 mM); Suspended solution; Need ultrasonic and warming and heat to 49°C
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.

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: 45% PEG300 5% Tween-80 50% Saline
Solubility: 10 mg/mL (11.51 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (11.51 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.95%

Fiche technique (279 KB) SDS (558 KB)

COA (250 KB) HNMR (220 KB) LCMS (139 KB) Elemental Analysis Report (107 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Souers AJ, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8. [Content Brief]

[2]. Peirs S, et al. ABT-199 mediated inhibition of BCL-2 as a novel therapeutic strategy in T-cell acute lymphoblastic leukemia. Blood. 2014 Dec 11;124(25):3738-47. [Content Brief]

[3]. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764. [Content Brief]

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Référence

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Cond.

Prix HT

Venetoclax [1257044-40-8]

Référence HY-15531-10mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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