l General Information |
Product Name | Pilaralisib (XL147) |
General description | Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. |
Synonym | SAR245408; 2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide |
Purity | ≥98.5%(HPLC) | CAS Number | 934526-89-3 |
Formula | C25H25ClN6O4S | Molecular Weight | 541.02 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | Solid |
Solubility(25°C) | DMSO | ≥50mg/ml |
Ethanol | Insoluble |
Water | Very slightly soluble |
l Biological Information |
Biochem/Physiol
Actions | Pilaralisib is an orally bioavailable small molecule, targeting the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity. Pilaralisib reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K signaling pathway; this may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents including genotoxic agents and receptor tyrosine kinase inhibitors. |
l Storage |
Storage temp. | -20°C |
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 |
