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(S)-JDQ-443

CAS No. : 2653994-10-4

MCE 站：(S)-JDQ-443

产品活性：(S)-JDQ-443 是 JDQ-443 (HY-139612)的异构体。JDQ-443 是一种口服有效和选择性的共价 KRAS G12C 抑制剂。JDQ-443 具有抗肿瘤活性。

研究领域：GPCR/G Protein  |  Cell Cycle/DNA Damage

作用靶点：Ras  |  PERK

In Vitro: JDQ-443 promotes dose-dependent reductions of phosphorylated ERK (pERK) levels ａnd the proliferation of the KRASG12C-mutated cell lines NCI-H358 ａnd NCI-H2122, with IC₅₀ values of 0.018 ａnd 0.063 μM, respectively.
JDQ443 covalently ａnd selectively binds ａnd inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, ａnd also inhibits proliferation of KRASG12C-mutated ａnd KRAS G12C/H95, G12C/R68S, ａnd G12C/Y96 double-mutant cell lines.

In Vivo: JDQ443 (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity ａnd inhibits the growth of tumor in a dose-dependent manner in KRAS G12C-mutated CDX models.
JDQ443 (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155.
JDQ443 generates categorical antitumor responses in PDX models of NSCLC ａnd colorectal tumors that are improved by combination treatment with other agents.

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