Panulisib
CAS号 | 1356033-60-7 | 货号 | BCP44105 |
中文名 | Panulisib | ||
英文名 | Panulisib | ||
中文别名 | |||
英文别名 | AK151761; AK 151761; AK-151761; P7170; P 7170; P-7170; | ||
分子式 | C27H20F3N9 | 分子量 | 527.5 |
生物活性 | Panulisib is a small molecule inhibitor of PI3K (IC50 = 2.2 nM) and mTOR (IC50 = 4.4 nM). It also inhibits ALK1 and DNA-PK, two important enzymes involved in angiogenesis and DNA repair with IC50 of 47 and 1.5 nM, respectively. P7170 inhibited PI3K-mTOR pathway proteins pAKT, pS6 and p4EBP1 by 90 to 100 % in Kras mutated NSCLC cell line (H460) in a western blot assay. P7170 also exhibited potent cytotoxicity activity against two Kras mutated NSCLC (H460 and A549) cell lines with IC50 values of 7 and 5 nM. P7170 by virtue of its unique profile represents an opportunity to deliver a first-in-class therapeutic option for patients saddled with Kras mutated non small cell lung cancer. | ||
信号通路 | PI3K/Akt/mTOR | ||
靶 点 | PI3K mTOR |
结构式
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