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KRAS inhibitor-10

CAS No. : 2578876-75-0

MCE 国际站：KRAS inhibitor-10

产品活性：KRAS inhibitor-10 选择性有效抑制 RAS 蛋白，特别是 KRAS 蛋白。KRAS inhibitor-10 是一种口服活性抗癌化合物，可用于癌症研究，如胰腺癌、乳腺癌、多发性骨髓瘤、白血病和肺癌。KRAS inhibitor-10 是一种四氢异喹啉化合物 (化合物 11)，详细信息请参考专利 WO2021005165 A1。

研究领域：GPCR/G Protein

作用靶点：Ras

In Vitro: KRAS inhibitor-10 (0.1-50 µΜ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRas^G12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRas^G12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas^G12D oncogenic mutation) and RPMI (myeloma cell line bearing KRas^G12A oncogenic mutation) cell proliferation with IC₅₀ values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively.
KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC₅₀ value is 0.413 μM.

In Vivo: KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10.

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