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ABT-199

(CAS No:1257044-40-8)

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. Phase 3.

CAS No:1257044-40-8

Molecular Weight(MW):868.44

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1257044-40-8
Molecular formula(MF)	C₄₅H₅₀ClN₇O₇S
Molecular Weight(MW):	868.44
Alias

Solubility

In vitro	DMSO	100 mg/mL warmed (115.14 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	5% DMSO+50% PEG 300+5% Tween 80+ddH2O	5mg/mL

Biological Activity

Description

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

Features

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

Targets

Bcl-2 ^[1] (Cell-free assay)	Bcl-xL ^[1] (Cell-free assay)	Bcl-w ^[1] (Cell-free assay)	Mcl-1 ^[1] (Cell-free assay)
<0.01 nM(Ki)	48 nM(Ki)	245 nM(Ki)	>444 nM(Ki)

In vitro

ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with K_i 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
RS4-11	Growth Inhibition Assay		72 h		IC50=0.0402 Î¼M	25649768
NALM-6	Growth Inhibition Assay		72 h		IC50>3 Î¼M	25649768
SU-DHL-6	Growth Inhibition Assay	0.8 Î¼M			Inhibits cell growth assessed by cell viability	25590803
OCI-Ly19	Growth Inhibition Assay	1 Î¼M			Inhibits cell growth assessed by cell viability	25590803
SU-DHL-6	Function Assay	0.75 Î¼M	18 h		Increases pro-survival protein MCL-1 expression	25590803
KCL22	Function Assay	2 Î¼M	48 h	DMSO	Increases DNA fragamentation	25333252
LOUCY	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=0.0139 Î¼M	25301704
ALL-SIL	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=0.1803 Î¼M	25301704
CUTLL1	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=0.3823 Î¼M	25301704
KOPTK1	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=0.6432 Î¼M	25301704
DND-41	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=1.9695 Î¼M	25301704
PF-382	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=2.1824 Î¼M	25301704
KARPAS-45	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=3.2225 Î¼M	25301704
PEER	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=4.6403 Î¼M	25301704
CX-1	Growth Inhibition Assay	100 Î¼M	72 h		IC50=6.7 Î¼M	25208882
LS147T	Growth Inhibition Assay	100 Î¼M	72 h		IC50=29.5 Î¼M	25208882
HL-60	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
MOLM-13	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
OCI-AML2	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
Kasumi-1	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
KG-1	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
THP-1	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
MOLM-14	Growth Inhibition Assay		48 h		IC50<1 Î¼M	24346116
MOLM-13	Apoptotic Assay	50 nM	24 h		Apoptosis induction	24346116
HSB	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=4.448 Î¼M	24342948
MOLT4	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=4.154 Î¼M	24342948
SKW-3/KE-37	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=0.712 Î¼M	24342948
SUPT-11	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=4.473 Î¼M	24342948
JURKAT	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=4.893 Î¼M	24342948
CCRF-CEM	Growth Inhibition Assay	10 Î¼M	48 h	DMSO	IC50=1.360 Î¼M	24342948
LOUCY	Apoptotic Assay	2 Î¼M	48 h	DMSO	Apoptosis induction	24342948

... Click to View More Cell Line Experimental Data

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]