An orally-available inhibitor of the B-raf mutant B-RafV600E
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PLX4720

Item No. 15142

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
CAS Number
918505-84-7
Synonyms
  • Raf Kinase Inhibitor V
Molecular Formula
C17H14ClF2N3O3S
Formula Weight
413.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.1 mg/mlEthanol: 2 mg/ml
λmax
214, 277 nm
SMILES
O=C(C1=C(F)C(NS(CCC)(=O)=O)=CC=C1F)C2=CNC3=NC=C(Cl)C=C32
InChi Code
InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22)
InChi Key
YZDJQTHVDDOVHR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).1 It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.1 PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.2,1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tsai, J., Lee, J.T., Wang, W., et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc. Natl. Acad. Sci. USA 105(8), 3041-3046 (2008).

    2. Nucera, C., Porrello, A., Antonello, Z.A., et al. B-RafV600E and thrombospondin-1 promote thyroid cancer progression. Proc. Natl. Acad. Sci. USA 107(23), 10649-10654 (2010).

    3. Nucera, C., Nehs, M.A., Nagarkatti, S.S., et al. Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. Oncologist 16(3), 296-309 (2011).