An inhibitor of B-RAF and C-RAF
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Belvarafenib

Item No. 31460

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-amino-N-[1-[(3-chloro-2-fluorophenyl)amino]-6-methyl-5-isoquinolinyl]-thieno[3,2-d]pyrimidine-7-carboxamide
CAS Number
1446113-23-0
Synonyms
  • GDC-5573
  • HM95573
Molecular Formula
C23H16ClFN6OS
Formula Weight
478.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml
λmax
215, 316 nm
SMILES
O=C(C1=CSC2=C1N=CN=C2N)NC3=C(C)C=CC4=C3C=CN=C4NC5=CC=CC(Cl)=C5F
InChi Code
InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29)
InChi Key
KVCQTKNUUQOELD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    Belvarafenib is an inhibitor of B-RAF and C-RAF (IC50s = 41, 7, and 2 nM for wild-type B-RAF, B-RAFV600E, and wild-type C-RAF, respectively).1 It is cytotoxic to B-RAFV600E-expressing A375 and SK-MEL-28 melanoma cells (IC50s = 57 and 69 nM, respectively), as well as COLO 205 and HCT116 colon and B-CPAP and CAL-62 thyroid cancer cells (IC50s = 116, 65, 43, and 479 nM, respectively). Belvarafenib reduces tumor growth in A375, SK-MEL-28, SK-MEL-2, and SK-MEL-30 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Man, R.-J., Zhang, Y.-L., Jiang, A.-Q., et al. A patent review of RAF kinase inhibitors (2010-2018). Expert Opin. Ther. Pat. 29(9), 675-688 (2019).