Product Name

Venetoclax

General description

Venetoclax is a Bcl-2-selective inhibitor.

Synonym

ABT-199; GDC-0199

Purity

≥99.0%(HPLC)

CAS Number

1257044-40-8

Formula

C⁴⁵H⁵⁰ClN⁷O⁷S

Molecular Weight

868.44

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Pale yellow to yellow or orange powder

Solubility(25℃)

DMSO

≥50mg/mL(warmed)

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Venetoclax is an orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia.

Venetoclax is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This  product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov