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编 号:F753883
分子式:C30H37N3O5
分子量:519.63
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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.Animal Model:Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice
Dosage:20 mg/kg
Administration:Oral administration; 20 mg/kg; BID; 27 days
Result:Decreased tumor volume and exhibited anti-tumor effects in the bearing mice.

体外研究:
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.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.
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