ABT 199
Tocris Bioscience, part of Bio-Techne | Catalog # 6960
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
Product Description
ABT 199 is a selective, high affinity Bcl-2 inhibitor (Ki < 0.010 nM). Exhibits >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1 (Ki > 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 (3CLpro) active site in a virtual screen. ABT 199 reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.Product Specifications
Molecular Weight
868.45
Formula
C45H50ClN7O7S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for ABT 199
For research use only
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