A B-Raf and VEGFR2 inhibitor
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RAF265

Item No. 16991

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amine
CAS Number
927880-90-8
Synonyms
  • CHIR265
Molecular Formula
C24H16F6N6O
Formula Weight
518.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
210, 266, 314 nm
SMILES
CN1C(NC2=CC=C(C(F)(F)F)C=C2)=NC3=C1C=CC(OC4=CC=NC(C5=NC=C(C(F)(F)F)N5)=C4)=C3
InChi Code
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)
InChi Key
YABJJWZLRMPFSI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $43

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    5 mg

    $183

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    10 mg

    $258

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    25 mg

    $483

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    Product Description

    RAF265 is a dual inhibitor of mutant B-RafV600E and vascular endothelial growth factor receptor 2 (EC50s = 0.14 and 0.19 µM, respectively, in cell-based assays).1 It can also inhibit wild-type B-Raf, platelet-derived growth factor receptor, colony-stimulating factor 1R, RET, c-KIT, SRC, and STE20 with IC50 values ranging from 20-100 nM.2 RAF265 can inhibit proliferation of melanoma and colorectal cancer cell lines with active BRAF mutations as well as suppress tumor growth in melanoma xenograft models bearing B-RafV600E mutations.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, T., Karsy, M., Zhuge, J., et al. B-Raf and the inhibitors: From bench to bedside. J. Hematol. Oncol. 6, 1-9 (2013).

    2. Su, Y., Vilgelm, A.E., Kelley, M.C., et al. RAF265 inhibits the growth of advanced human melanoma tumors. Clin. Cancer Res. 18(8), 2184-2198 (2012).