An inhibitor of mutant V600E and wild type B-Raf
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PLX4032

Item No. 10618

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
CAS Number
918504-65-1
Synonyms
  • RG-7204
  • Ro 51-85426
  • Vemurafenib
Molecular Formula
C23H18ClF2N3O3S
Formula Weight
489.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 1 mg/ml
λmax
219, 252, 307 nm
SMILES
ClC1=CC=C(C2=CN=C(NC=C3C(C4=C(F)C=CC(NS(=O)(CCC)=O)=C4F)=O)C3=C2)C=C1
InChi Code
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
InChi Key
GPXBXXGIAQBQNI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $49

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    25 mg

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    Product Description

    PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively).1 It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells.1 PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.2,3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Khazak, V., Astsaturov, I., Serebriiskii, I.G., et al. Selective Raf inhibition in cancer therapy. Expert Opin. Ther. Targets 11(12), 1587-1609 (2007).

    2. Flaherty, K.T., Puzanov, I., Kim, K.B., et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N. Engl. J. Med. 363(9), 809-819 (2010).

    3. Bollag, G., Hirth, P., Tsai, J., et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 467(7315), 596-599 (2010).

    4. Coffee, E.M., Faber, A.C., Roper, J., et al. Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAFV600E colorectal cancer. Clin. Cancer Res. 19(10), 2688-2698 (2013).

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