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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1628838-42-5
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1313.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥450.0 |
| 规格： | 5 mg | 产品价格： | ￥1100.0 |
| 规格： | 10 mg | 产品价格： | ￥1800.0 |
| 规格： | 25 mg | 产品价格： | ￥3338.0 |
| 规格： | 50 mg | 产品价格： | ￥4929.0 |
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RAF709
CAS No. : 1628838-42-5
MCE 国际站：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.
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