Divarasib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Divarasib (GDC-6036) 是一种具有口服生物利用度，选择性的 KRAS G12C 抑制剂，IC50 为 <0.01 μM。Divarasib 与 KRAS G12C 的开关 II (SW-II) 口袋共价结合，并将其不可逆地锁定在非活动的 GDP 结合状态。

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.

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Animal Model:Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cellsDosage: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.

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Others

Other Targets

Kras

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2417987-45-0

622.06

C29H32ClF4N7O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (160.76 mM; 超声助溶 )

C[C@H]1CN(CCN1c1nc(OC[C@@H]2CCCN2C)nc2c(F)c(c(Cl)cc12)-c1nc(N)cc(C)c1C(F)(F)F)C(=O)C=C

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(-20℃)

With Ice Pack

≥ 2 years