RAF709 是一种有效的 RAF 抑制剂，抑制 BRAF 和 CRAF，IC₅₀ 分别为 0.4 nM 和 0.5 nM。具有抗肿瘤活性。

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC 50 s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.

Solid

CRAF 0.5 nM (IC50) Braf 0.4 nM (IC50

RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709 shows dose-proportional increases in plasma exposure and a corresponding dosedependent inhibition of pERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kg being subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200 mg/kg results in mean tumor regression of 92%, while the same high dose is not efficacious in the PC3, KRAS WT model. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Nishiguchi GA, et al. Design and Discovery of N-(2-Methyl-5-morpholino-6-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med

In Vitro: DMSO : 100 mg/mL (184.31 mM; Need ultrasonic and warming)配制储备液