ABT 199

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Cat.No. 6960 - ABT 199 | C45H50ClN7O7S | CAS No. 1257044-40-8
Description: Selective, high affinity Bcl-2 inhibitor; orally bioavailable
Alternative Names: 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)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

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.

Technical Data

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

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

Preparing Stock Solutions

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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References

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


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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, GDC-0199, Family, 6960, Tocris Bioscience

Citations for ABT 199

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Literature in this Area

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Programmed Cell Death

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

Apoptosis

Apoptosis Signaling Pathway

Apoptosis is a physiological process for cell death that is critical during aging and development. It may also be referred to as cell 'suicide'. Apoptosis can be triggered by events both inside and outside of the cell.