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。
货号:ajcx33816
CAS:2578876-75-0
分子式:C30H37N3O5
分子量：519.63
溶解度:DMSO : 100 mg/mL (192.44 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1[1].

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 KRasG12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRasG12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRasG12D oncogenic mutation) and RPMI (myeloma cell line bearing KRasG12A oncogenic mutation) cell proliferation with IC50 values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively[1].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[1].

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[1].

[1]. Miguel VEGA GARCÍA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165