产品
编 号：F741582
分子式：C29H32ClF4N7O2
分子量：622.06
分子式：C29H32ClF4N7O2
分子量：622.06
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2417987-45-0
产品详情
生物活性：
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
体内研究：
Divarasib (10-100 mg/kg/天；PO，持续 7 天) 降低游离 KRAS G12C 的比例。Animal Model:Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cells
Dosage:10, 25, or 100 mg/kg
Administration:Oral gavage (PO) every day (QD) for 7 days (vehicle: 0.5% methylcellulose)
Result:Decreased the ratio of free KRAS G12C to internal standard. Dose-dependent target engagement was observed for all time points (2, 8, and 24 h post-last dose), with over 90% KRAS G12C engagement observed for the highest dose 100 mg/kg assessed.
体外研究：
Divarasib (化合物 17a) 在 K-Ras G12C-烷基化 HCC1171 细胞中的 EC50 为 2 nM。
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
体内研究：
Divarasib (10-100 mg/kg/天；PO，持续 7 天) 降低游离 KRAS G12C 的比例。Animal Model:Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cells
Dosage:10, 25, or 100 mg/kg
Administration:Oral gavage (PO) every day (QD) for 7 days (vehicle: 0.5% methylcellulose)
Result:Decreased the ratio of free KRAS G12C to internal standard. Dose-dependent target engagement was observed for all time points (2, 8, and 24 h post-last dose), with over 90% KRAS G12C engagement observed for the highest dose 100 mg/kg assessed.
体外研究：
Divarasib (化合物 17a) 在 K-Ras G12C-烷基化 HCC1171 细胞中的 EC50 为 2 nM。
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