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Submit ReviewABT 199
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)
Biological Activity for ABT 199
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.
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 Data for ABT 199
| 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 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 | 2.3 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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Product Datasheets for ABT 199
References for ABT 199
References are publications that support the biological activity of the product.
Souers et al (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat.Med. 19 202 PMID: 23291630
Soderquist et al (2018) Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity. Nat.Commun. 9 3513 PMID: 30158527
Liu et al (2019) Balancing apoptosis and autophagy for Parkinson's disease therapy: targeting BCL-2. ACS Chem.Neurosci. 10 792 PMID: 30400738
Bosc et al (2021) Mitochondrial inhibitors circumvent adaptive resistance to venetoclax and cytarabine combination therapy in acute myeloid leukemia. Nat.cancer 2 1204 PMID: 35122057
If you know of a relevant reference for ABT 199, please let us know.
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Keywords: ABT 199, ABT 199 supplier, ABT199, GDC, 0199, GDC0199, Bcl-2, inhibitors, inhibits, induces, apoptosis, orally, bioavailable, selective, high, affinity, SARS-CoV-2, 3C-like, protease, severe, acute, respiratory, syndrome, coronavirus, COVID-19, Venetoclax, GDC-0199, Family, 3C, and, 3CL, Proteases, 6960, Tocris Bioscience
1 Citation for ABT 199
Citations are publications that use Tocris products. Selected citations for ABT 199 include:
Håkon et al (2020) Targeting Cellular Metabolism in Acute Myeloid Leukemia and The Role of Patient Heterogeneity. Cells 9 PMID: 32392896
Do you know of a great paper that uses ABT 199 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Pathways for ABT 199
