ARS-853

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ARS-853

CAS No. : 1629268-00-3

MCE 国际站：ARS-853

产品活性：ARS-853 是选择性，共价的 KRAS G12C 抑制剂，IC₅₀ 为 2.5 μM。ARS-853 通过与 GDP 结合的癌蛋白结合并阻止激活来抑制突变 KRAS 驱动的信号传导。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Ras  |  Apoptosis

In Vitro: ARS853 is designed to bind KRAS^G12C with high affinity. Treatment of KRAS^G12C-mutant lung cancer cells with ARS853 reduces the level of GTP-bound KRAS by more than 95% (10 μM). ARS853 inhibits proliferation with an inhibitory concentration 50% (IC₅₀) of 2.5 μM, which is similar to its IC₅₀ for target inhibition. ARS853 (10 μM) inhibits effector signaling and cell proliferation to varying degrees in six KRAS^G12C mutant lung cancer cell lines, but not in non-KRAS^G12C models. Similarly, it completely suppresses the effects of exogenous KRAS^G12C expression on KRAS-GTP levels, KRAS-BRAF interaction, and ERK signaling. ARS-853 treatment also induces apoptosis in four KRAS^G12C mutant cell lines. ARS853 selectively reduces KRAS-GTP levels and RAS-effector signaling in KRAS^G12C-mutant cells, while inhibiting their proliferation and inducing cell death. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.

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