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RAF709

CAS No. : 1628838-42-5

MCE 站：RAF709

产品活性：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。

研究领域：MAPK/ERK Pathway

作用靶点：Raf

In Vitro: 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Doramapimod  |  GW 5074  |  Ro 5126766  |  AZ 628  |  GDC-0879  |  ZM 336372  |  Agerafenib  |  Raf inhibitor 1  |  AZ304  |  L-779450  |  MCP110  |  Sorafenib (D3)  |  Raf inhibitor 2

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