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  • RAF709
RAF709的可视化放大

RAF709

A potent inhibitor of B-RAF and C-RAF

原价
¥912-6462
价格
730-5170
RAF709的二维码

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  • 库存: 现货
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  • 货号: ajci22856
  • CAS: 1628838-42-5
  • 别名:
  • 分子式: C28H29F3N4O4
  • 分子量: 542.55
  • 纯度: >98%
  • 溶解度: DMSO : 100 mg/mL (184.31 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].


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[1].


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[1].


参考文献:
[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 Chem. 2017 Jun 22;60(12):4869-4881.

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