ABT 199

Name: ABT 199
Brand: Tocris Bioscience
SKU: 6960

Tocris Bioscience, part of Bio-Techne | Catalog # 6960

Citations (10)

COA / SDS

Selective, high affinity Bcl-2 inhibitor; orally bioavailable

Key Product Details

Description:	Selective, high affinity Bcl-2 inhibitor; orally bioavailable
Alternative Names:	Venetoclax,GDC-0199
Chemical Name:	4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
Purity:	≥98% (HPLC)
Molecular Weight:	868.45

View Full Technical Details for ABT 199

Technical Data
Citations

Biological Activity for ABT 199

ABT 199 is a selective, high affinity Bcl-2 inhibitor (K_i < 0.010 nM). Exhibits >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1 (K_i > 444 nM). Potently induces apoptosis in FL5.12-BCL-2 cells (EC₅₀ = 261 nM) and reduces tumor burden in chronic lymphocytic leukemia (CLL) primary samples (EC₅₀ = 3 nM). Shows reduced toxicity to platelets compared to similar compounds. Enhances efficacy of clinically relevant chemotherapy and immunotherapy drugs. Orally bioavailable. Exhibits binding to SARS-CoV-2 3C-like protease (3CL^pro) active site in a virtual screen. ABT 199 reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.

Compound Libraries for ABT 199

ABT 199 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for ABT 199

M. Wt	868.45
Formula	C₄₅H₅₀ClN₇O₇S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1257044-40-8
PubChem ID	49846579
InChi Key	LQBVNQSMGBZMKD-UHFFFAOYSA-N
Smiles	CC1(C)CCC(CN2CCN(CC2)C2=CC(OC3=CN=C4NC=CC4=C3)=C(C=C2)C(=O)N[S](=O)(=O)C2=CC(=C(NCC3CCOCC3)C=C2)[N](=O)=O)=C(C1)C1=CC=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for ABT 199

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	86.84	100

Preparing Stock Solutions for ABT 199

The following data is based on the product molecular weight 868.45.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.30 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

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References for ABT 199

References are publications that support the biological activity of the product.

Bosc Mitochondrial inhibitors circumvent adaptive resistance to venetoclax and cytarabine combination therapy in acute myeloid leukemia. Nat.cancer 2021 PMID: 35122057
Soderquist Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity. Nat.Commun. 2018 PMID: 30158527
Liu Balancing apoptosis and autophagy for Parkinson's disease therapy: targeting BCL-2. ACS Chem.Neurosci. 2019 PMID: 30400738
Souers ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat.Med. 2013 PMID: 23291630