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RAF265

Chemical Structure : RAF265

CAS No.: 927880-90-8

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

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 518.4139
Formula C24H16F6N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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]-

References

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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