CAS NO: | 1173204-81-3 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | PKI-402 is a selective, reversible, ATP-competitive inhibitor ofPI3K, including PI3K-α mutants, andmTOR(IC50=2, 3, 7,14 and 16 nM forPI3Kα,mTOR,PI3Kβ,PI3Kδand PI3Kγ). | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | PKI-402 is an equipotent inhibitor of class I PI3K, including the E545K and H1047R PI3K-α mutants (IC50=2, 3 and 3 nM for PI3Kα, PI3Kα-H1047R and PI3Kα-E545K, respectively). PKI-402 causes in vitro growth inhibition of human tumor cell lines derived from a diverse set of human tumor tissues, including breast, brain (glioma), pancreas, and non-small cell lung cancer (NSCLC) tissues. PKI-402 inhibits MDA-MB-361 [breast: Her2+andPIK3CAmutant (E545K)], with an IC50of 6 nM. PKI-402 inhibits HCT116 (K-Ras andPIK3CAmutant) with an IC50of 33 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | PKI-402 displays antitumor activity (i.v. route) in breast [MDA-MB-361: Her2+and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models. PKI-402 causes regression in the MDA-MB-361 xenograft model. PKI-402 effect is most pronounced at 100 mg/kg (daily for 5 days, one round), which reduces initial tumor volume and prevents tumor re-growth for 70 days. In MDA-MB-361 tumor tissue, PKI-402 at 100 mg/kg (single dose) fully suppresses p-Akt at both the T308 and the S473 sites at 8 hours and induces cleaved PARP. At 24 hours, p-Akt suppression is still evident, as is cleaved PARP[1]. | ||||||||||||||||
分子量 | 570.65 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H34N10O3 | ||||||||||||||||
CAS 号 | 1173204-81-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 5 mg/mL(8.76 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |