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Venetoclax (ABT-199)

Name: Venetoclax (ABT-199)
Brand: Selleck Chemicals
SKU: S8048
Rating: 5 (535 reviews)

Synonyms: GDC-0199

Catalog No.S8048 Purity: 99.97%

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. 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.

Venetoclax (ABT-199) Chemical Structure

CAS: 1257044-40-8

Selleck's Venetoclax (ABT-199) has been cited by 535 publications

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Products often used together with Venetoclax (ABT-199)

A-1331852

Venetoclax and A-1331852, when used in combination with nilotinib, synergistically reduce cell viability, and enhance apoptosis in blast phase-chronic myeloid leukemia cell lines.

Parry N, et al. Cell Death Discov. 2022 Nov 15;8(1):457.

Azacitidine (5-Azacytidine)

Combining Venetoclax and Azacitidine targets leukemia stem cells and disrupts abnormal energy metabolism in AML patients with poor outcomes.

Pollyea DA, et al.Nat Med. 2018 Dec;24(12):1859-1866.

A-1210477

Venetoclax and A-1210477 increase MCL1 expression and synergistically induce apoptosis in acute myeloid leukemia (AML) cells, MOLM13/MV4-11/SKM1/OCI-AML5.

Fiskus W, et al. Blood Cancer J. 2019 Jan 15;9(2):4.

Navitoclax (ABT-263)

Venetoclax, Navitoclax and chemotherapy show promising efficacy and tolerability in patients with relapsed/refractory acute lymphoblastic leukemia.

Pullarkat VA, et al. Cancer Discov. 2021 Jun;11(6):1440-1453.

S63845

Venetoclax and S63845 significantly delay the time to viral rebound by 4-fold after antiretroviral therapy (ART) cessation in a humanized mouse model of HIV-1 infection.

Arandjelovic P, et al. Cell Rep Med. 2023 Aug 23;101178.

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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 μM	25649768
NALM-6	Growth Inhibition Assay		72 h		IC50>3 μM	25649768
SU-DHL-6	Growth Inhibition Assay	0.8 μM			Inhibits cell growth assessed by cell viability	25590803
OCI-Ly19	Growth Inhibition Assay	1 μM			Inhibits cell growth assessed by cell viability	25590803
SU-DHL-6	Function Assay	0.75 μM	18 h		Increases pro-survival protein MCL-1 expression	25590803
KCL22	Function Assay	2 μM	48 h	DMSO	Increases DNA fragamentation	25333252
LOUCY	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=0.0139 μM	25301704
ALL-SIL	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=0.1803 μM	25301704
CUTLL1	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=0.3823 μM	25301704
KOPTK1	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=0.6432 μM	25301704
DND-41	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=1.9695 μM	25301704
PF-382	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=2.1824 μM	25301704
KARPAS-45	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=3.2225 μM	25301704
PEER	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=4.6403 μM	25301704
CX-1	Growth Inhibition Assay	100 μM	72 h		IC50=6.7 μM	25208882
LS147T	Growth Inhibition Assay	100 μM	72 h		IC50=29.5 μM	25208882
HL-60	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
MOLM-13	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
OCI-AML2	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
Kasumi-1	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
KG-1	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
THP-1	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
MOLM-14	Growth Inhibition Assay		48 h		IC50<1 μM	24346116
MOLM-13	Apoptotic Assay	50 nM	24 h		Apoptosis induction	24346116
HSB	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=4.448 μM	24342948
MOLT4	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=4.154 μM	24342948
SKW-3/KE-37	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=0.712 μM	24342948
SUPT-11	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=4.473 μM	24342948
JURKAT	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=4.893 μM	24342948
CCRF-CEM	Growth Inhibition Assay	10 μM	48 h	DMSO	IC50=1.360 μM	24342948
LOUCY	Apoptotic Assay	2 μM	48 h	DMSO	Apoptosis induction	24342948
RS4:11	Cytotoxicity assay					29407973
RS4:11	MTS assay		72 h			30278333
RS4:11	MTS assay					28926247
Toledo	MTS assay		72 h			30278333
NCI60	SRB assay		48 h			27994761
RS4:11	MTT assay		24 h			29453135
melanoma	SRB assay		48 h			27994761
leukemia	SRB assay		48 h			27994761
renal cancer	SRB assay		48 h			27994761
non-small cell lung cancer	SRB assay		48 h			27994761
breast cancer	SRB assay		48 h			27994761
colon cancer	SRB assay		48 h			27994761
ovarian cancer	SRB assay		48 h			27994761
CNS cancer	SRB assay		48 h			27994761
prostate cancer	SRB assay		48 h			27994761
Remb1	MTT assay		24 h			29453135
Click to View More Cell Line Experimental Data

Biological Activity

Description

Features

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

Targets

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

<0.01 nM(Ki)

In vitro
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]
Kinase Assay	Binding affinity assays
Kinase Assay	Binding affinities (K_i or IC50) of ABT-199 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-199 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters.
Cell Research	Cell lines	NHL, DLBCL, MCL, AML and ALL cell lines
	Concentrations	~1 μM
	Incubation Time	48 hours
	Method	RS4;11 cells are seeded at 5 × 10⁴ per well in 96-well plates and treated with ABT-199 diluted in half-log steps starting at 1 μM-0.05 nM. Leukemia and lymphoma cell lines are seeded at 1.5-2 × 10⁴ cells per well in the appropriate medium and incubated with ABT-199 for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration-response data.
Experimental Result Images	Methods	Biomarkers	Images	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
	Immunofluorescence	Bcl-2 / Mcl-1		28767232

In Vivo
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]
Animal Research	Animal Models	Female C.B-17 SCID mice (DoHH2 and Granta-519 xenografts) and female C.B-17 SCID-beige mice (RS4;11 and Toledo xenografts)
	Dosages	~100 mg/kg
	Administration	Orally

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05668026	Not yet recruiting	HIV-1-infection	University of Aarhus\|The Peter Doherty Institute for Infection and Immunity\|Walter and Eliza Hall Institute of Medical Research\|The Alfred\|Aarhus University Hospital	March 1 2024	Phase 1\|Phase 2
NCT06191263	Not yet recruiting	Acute Myeloid Leukemia	Ryvu Therapeutics SA	January 2024	Phase 2
NCT06014489	Not yet recruiting	AML Adult	Stichting Hemato-Oncologie voor Volwassenen Nederland	December 2023	Phase 2

References

[1] Souers AJ, et al. Nat Med, 2013, 19(2), 202-208.

Chemical lnformation & Solubility

Molecular Weight	868.44	Formula	C₄₅H₅₀ClN₇O₇S
CAS No.	1257044-40-8	SDF	Download Venetoclax (ABT-199) SDF
Smiles	CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (115.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 Corn oil	2.5mg/ml (2.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O	1.8mg/ml (2.07mM)	Taking the 1 mL working solution as an example, add 100 μL of 18 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 50%PEG300 2 5%Tween80 3 40%ddH2O	2.5mg/ml (2.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 500 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 400 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
Could you please offer some advice on the half-life of the drug ?

Answer:
According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.

Bcl-2 Signaling Pathway Map

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):