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Product Details

PLX-4032 | BRAF inhibitor

PLX-4032 (918504-65-1) is an ATP-competitive inhibitor of mutant V600E/F and wild type B-Raf, IC50s=31 and 100 nM respectively.1 Induced growth inhibition, G0/G1 arrest and apoptosis in a variety of cancer cell lines, with a B-Raf mutation favoring but not guaranteeing a response.2 Inhibits the growth of B-Raf V600E-positive melanomas in vitro and in vivo.3 Treatment of patients that carry the V600E BRAF mutation resulted in complete or partial tumor regression.4

References/Citations

1) Khazak et al. (2007), Selective Raf inhibition in cancer therapy; Expert Opin. Ther. Targets, 11 1587
2) Tap et al. (2010), Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma; Neoplasia, 12 637
3) Lee et al. (2010), PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas; Pigment Cell Melanoma Res., 23 820
4) Flaherty et al. (2010), Inhibition of mutated, activated BRAF in metastatic melanoma; N. Engl. J. Med., 363 809

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Catalog#  10-2928-0005

$40.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
918504-65-1
Catalog Number:
10-2928
Activity:
BRAF inhibitor
Chemical Name:
N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
Alternate Names:
Vemurafenib, R7204, Ro 51-85426
Molecular Weight:
489.92
Molecular Formula:
C23H18ClF2N3O3S
Solubility:
Soluble in DMSO (up to 100 mg/ml)
Physical Properties:
White or off-white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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