Venetoclax (ABT-199)

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

Keywords

Venetoclax (ABT-199) GDC-0199 1257044-40-8

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Biological Activity

Description

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.

Features

Re-engineered version of ABT-263 (Navitoclax).

Targets

Bcl-2 [1]
(Cell-free assay)

<0.01 nM(Ki)

In vitro

ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM. [1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
CS-THL1	Growth Inhibition Assay	20 nM	72 h	DMSO	Inhibits cell growth assessed by cell viability	25916698
CS-THL1	Apoptotic Assay	25 nM		DMSO	Induces apoptosis	25916698
DoGKiT	Apoptotic Assay	50 nM		DMSO	Induces apoptosis	25916698

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Mcl-1 / Bcl-xl / Bcl-2 / Bak / NOXA / Bim; PARP / Cleaved PARP / Caspase 3 / Cleaved caspase3 / p-S6(Ser236/236);	30663221
Growth inhibition assay	Cell death; Cell viability;	28714472 29876007
Immunofluorescence	Bcl-2 / Mcl-1;	28767232

In vivo

ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents. [1]

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