PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

Solid

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 体外研究 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 and PIK3CA mutant (E545K)], with an IC₅₀ of 6 nM. PKI-402 inhibits HCT116 (K-Ras and PIK3CA mutant) with an IC₅₀ of 33 nM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature or refrigerated transportation.

• [1]. Mallon R et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.  [Information]

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。