RAF265

• CAT Number: I005517
• CAS Number: 927880-90-8
• Molecular Formula: C₂₄H₁₆F₆N₆O
• Molecular Weight: 518.41
• Purity: ≥95%
• Target: VEGFR
• Solubility: DMSO: ≥ 26 mg/mL
• Storage: 3 years -20C powder
• IC50: 3-60 nM (B-Raf); 30 nM(EC50 for VEGFR2)
• InChI: InChI=1S/C24H16F6N6O/c1-36-19-7-6-15(10-17(19)34-22(36)33-14-4-2-13(3-5-14)23(25,26)27)37-16-8-9-31-18(11-16)21-32-12-20(35-21)24(28,29)30/h2-12H,1H3,(H,32,35)(H,33,34)
• InChIKey: YABJJWZLRMPFSI-UHFFFAOYSA-N
• SMILES: CN1C2=C(C=C(C=C2)OC3=CC(=NC=C3)C4=NC=C(N4)C(F)(F)F)N=C1NC5=CC=C(C=C5)C(F)(F)F

RAF265 (Cat No.:I005517), also known as (CHIR-265), is an arylamino benzimidazole-based inhibitor of B-RAF, C-RAF and VEGFR2.With an IC50 of 3-60 nM and exhibiting potent inhibition of VEGFR2 phosphorylation, RAF265 (CHIR-265) induces cell cycle blockage and apoptosis.

Reference

[1]. AACR Meeting Abstracts 2008;2008:4876.


[2]. Mordant P, et al. Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination. Mol Cancer Ther, 2010, 9(2), 358-368.


[3]. Zitzmann K, et al. The novel Raf inhibitor Raf265 decreases Bcl-2 levels and confers TRAIL-sensitivity to neuroendocrine tumour cells. Endocr Relat Cancer, 2011, 18(2), 277-285.


[4]. Tseng JR, et al. Use of DNA microarray and small animal positron emission tomography in preclinical drug evaluation of RAF265, a novel B-Raf/VEGFR-2 inhibitor. Neoplasia, 2011, 13(3), 266-275.