Product Name

Apitolisib (GDC-0980, RG7422)

General description

Apitolisib is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ.

Synonym

(2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2 hydroxypropan-1-one

Purity

≥98.0%(HPLC)

CAS Number

1032754-93-0

Formula

C²³H³⁰N⁸O³S

Molecular Weight

498.6

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥15mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Apitolisib is an orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Apitolisib inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. 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 in a PI3K-independent fashion.

Apitolisib is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases.

Application

Apitolisib has been used in trials studying the treatment of Solid Cancers, Breast Cancer, Prostate Cancer, Renal Cell Carcinoma, and Endometrial Carcinoma, 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