Product Name

Dactolisib (BEZ235, NVP-BEZ235)

General description

Dactolisib is an orally bioavailable imidazoquinoline targeting the phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

Synonym

2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile; NVP-BEZ 235

Purity

≥98.0%(HPLC)

CAS Number

915019-65-7

Formula

C³⁰H²³N⁵O

Molecular Weight

469.55

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

Very slightly soluble

DMF

≥15mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Dactolisib is an orally bioavailable imidazoquinoline targeting the phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. Dactolisib inhibits PI3K kinase and mTOR kinase in the PI3K/AKT/mTOR kinase signaling pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K/mTOR-overexpressing tumor cells. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Dactolisib is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

Application

Dactolisib has been used in trials studying the treatment of Cancer, Solid Tumor, Renal Cancer, Breast Cancer, and Cowden Syndrome, among others.

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