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Izorlisib

CAS No. : 1007207-67-1

MCE 站：Izorlisib

产品活性：Izorlisib (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: Izorlisib (CH5132799) is a selective class I PI3K inhibitor with potent antitumor activity against tumors harboring the PIK3CA mutations. Izorlisib selectively inhibits class I PI3Ks ａnd PI3Kα mutants in in vitro kinase assays. Izorlisib 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), Izorlisib is shown to interact with ATP-binding sites of the enzyme, suggesting an ATP competitive mode of inhibition. No significant inhibitory activities of Izorlisib are observed against a representative panel of 26 protein kinases, including RTKs, nonreceptor tyrosine kinases, ａnd serine/threonine kinases. These data indicate that Izorlisib is a selective class I PI3K inhibitor, especially against PI3Kα ａnd its mutants. Izorlisib 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 Izorlisib 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. Izorlisib 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. Izorlisib 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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