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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-RAF265
RAF265

Chemical Structure : RAF265

CAS No.: 927880-90-8

RAF265 (CHIR-265;RAF 265;RAF-265;CHIR265)

货号: PC-42483Not For Human Use, Lab Use Only.

RAF265 (CHIR265) is a potent, oral, dual Raf/VEGFR-2 inhibitor with IC50 of 3-60 nM for C-Raf/B-Raf/B-Raf V600E, EC50 of 30 nM for VEGFR2 phosphorylation.

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10 mg ¥1880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RAF265 (CHIR265) is a potent, oral, dual Raf/VEGFR-2 inhibitor with IC50 of 3-60 nM for C-Raf/B-Raf/B-Raf V600E, EC50 of 30 nM for VEGFR2 phosphorylation.
RAF265 (CHIR265) blocks Raf-MEK-ERK signalling and significantly enhances TRAIL sensitivity in NCI-H727 and CM insulinoma cells.
RAF265 (CHIR265) inhibits cell proliferation with IC50 of 0.83-5.54 uM in CRC cells, demonstrates significant anti-tumor activity in tumors of xenograft models.

物理化学性质&存储条件

分子量 518.4139
分子式 C24H16F6N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 26 mg/mL

Chemical Name/SMILES

1H-Benzimidazol-2-amine, 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-

参考文献

1. Mordant P, et al. Mol Cancer Ther. 2010 Feb;9(2):358-68.

2. Zitzmann K, et al. Endocr Relat Cancer. 2011 Mar 21;18(2):277-85.

3. Su Y, et al. Clin Cancer Res. 2012 Apr 15;18(8):2184-98.

4. Chen J, et al .Cancer Res. 2011 Jun 15;71(12):4280-91.

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