l General Information |
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 |