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CH5132799

CAS No. : 1007207-67-1

MCE 站：CH5132799

产品活性：CH5132799 是一种选择性的 I 类 PI3K 抑制剂。抑制 PI3Kα, IC₅₀ 为 14 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: CH5132799 is a selective class I PI3K inhibitor with potent antitumor activity against tumors harboring the PIK3CA mutations. CH5132799 selectively inhibits class I PI3Ks ａnd PI3Kα mutants in in vitro kinase assays. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC₅₀ of 14 nM. IC₅₀ values against class II PI3Ks (C2α ａnd C2β), a class III PI3K (Vps34), ａnd a class IV PI3K (mTOR) are more than 100-fold higher than that against PI3Kα. Interestingly, slightly lower IC₅₀ values are observed against PI3Kα with oncogenic mutations E542K, E545K, ａnd H1047R than against wild-type (WT) PI3Kα. In an analysis of cocrystal structure with PI3Kγ (PBD ID: 3APC), CH5132799 is shown to interact with ATP-binding sites of the enzyme, suggesting an ATP competitive mode of inhibition. No significant inhibitory activities of CH5132799 are observed against a representative panel of 26 protein kinases, including RTKs, nonreceptor tyrosine kinases, ａnd serine/threonine kinases. These data indicate that CH5132799 is a selective class I PI3K inhibitor, especially against PI3Kα ａnd its mutants. CH5132799 shows superior antiproliferative activity across the 4 tumor types, with 75% (45/60) of lines having an IC₅₀ below 1 μM ａnd 38% (23/60) of lines having an IC₅₀ below 0.3 μM.

In Vivo: Mice bearing BT-474 tumors (n=14) are orally administered 50 mg/kg of Everolimus on a daily basis for 31 days ａnd then randomized. After randomization, the mice are orally administered 50 mg/kg of Everolimus (n=4) ａnd 12.5 mg/kg (n=5), ａnd 25 mg/kg (n=5) of CH5132799 on a daily basis for 7 days. C, the vehicle-, Everolimus, ａnd CH5132799-treated (25 mg/kg) tumors are resected at 4 hours after terminal administration in B, lysed, ａnd analyzed by Western blotting. CH5132799 administration leads to a remarkable regression in a dose-dependent manner of the tumors regrown after the long-term Everolimus treatment. The tumors are resected at the end of treatment ａnd analyzed by Western blotting with respect to PI3K pathway inhibition. CH5132799 suppresses various effectors in the PI3K pathway, including Akt, FoxO1, S6K, S6, ａnd 4E-BP1, whereas Everolimus inhibits only phosphorylation of S6K ａnd S6, both downstream effectors of mTORC1.

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