PLX4032 | BRAF inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $40.00 | ||
| 25 mg | $145.00 |
PLX4032 (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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
PLX4032 (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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