Bioactivity | PI3Kα-IN-21 (compound 8) is a PI3Kα inhibitor, and its selectivity for PI3Kα is 10.41/16.99/37.53 times higher than PI3Kβ/γ/δ respectively (IC50: 96.89/568.24/397.48 nM ). PI3Kα-IN-21 inhibits cancer cell activity, proliferation, and migration, and induces mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. PI3Kα-IN-21 exhibits in vivo antitumor potency in a mouse model of non-small cell lung cancer[1]. |
Target | IC50: 56 nM (PI3Kα), 96.89 nM (PI3Kβ), 568.24 nM (PI3Kγ), 397.48 nM nM (PI3Kδ) |
Formula | C38H30N4O |
Molar Mass | 558.67 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Liu C, et al. Hybridization-based discovery of novel quinazoline-2-indolinone derivatives as potent and selective PI3Kα inhibitors. J Adv Res. 2024 Mar 11:S2090-1232(24)00089-4. |