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.
性状
Solid
IC50 & Target[1][2]
KRas G12C
体外研究(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 oncogenic mutation), H358 (non-small cell lung cancer line bearing KRas oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas oncogenic mutation) and RPMI (myeloma cell line bearing KRas 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Miguel VEGA GARCíA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165
溶解度数据
In Vitro: DMSO : 100 mg/mL (192.44 mM; Need ultrasonic)配制储备液