Vemurafenib (PLX4032, RG7204)

Vemurafenib (PLX4032, RG7204)

Catalog Number:
L002368463APE
Mfr. No.:
APE-A3004
Price:
$188
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          Vemurafenib is an inhibitor of BRAF kinase. It inhibits BRAFV600E and also has inhibitory activity in vitro against several other kinds of kinases, including CRAF, ARAF and wild-type BRAF. Vemurafenib is a competitive small-molecule serine–threonine kinase inhibitor that functions by binding to the ATP-binding domain of mutant BRAF. Vemurafenib can also give rise to activation of downstream MEK by normal RAF homo- and heterodimers in non-BRAF mutated cells, which has been shown to be caused by transactivation of the nondrug-bound partner in BRAF to CRAF heterodimers and CRAF to CRAF homodimers.

      • Properties
        • Alternative Name
          Vemurafenib, Zelboraf, PLX-4032, RG7204, RO5185426; N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
          CAS Number
          918504-65-1
          Molecular Formula
          C23H18ClF2N3O3S
          Molecular Weight
          489.93
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥24.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
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          2. Satoh TK, Mellett M, et al. "IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes." J Clin Invest. 2019 Dec 5. pii: 128678. PMID:31805013
          3. Sechi M, Lall RK, et al. "Fisetin targets YB-1/RSK axis independent of its effect on ERK signaling:insights from in vitro and in vivo melanoma models." Sci Rep. 2018 Oct 24;8(1):15726. PMID:30356079
          4. Zanconato F, Battilana G, et al. "Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4." Nat Med. 2018 Oct;24(10):1599-1610. PMID:30224758
          5. Hwang BJ, Adhikary G, et al. "Chk1 inhibition as a novel therapeutic strategy in melanoma." Oncotarget. 2018 Jul 13;9(54):30450-30464. PMID:30100999
          6. Talebi A, Dehairs J, et al. "Sustained SREBP-1-dependent lipogenesis as a key mediator of resistance to BRAF-targeted therapy." Nat Commun.2018 Jun 27;9(1):2500. PMID:29950559
          7. Zuo Q, Liu J, et al. "AXL/AKT axis mediated-resistance to BRAF inhibitor depends on PTEN status in melanoma."Oncogene. 2018 Mar 19. PMID:29551771
          8. Fisher ML, Grun D, et al. "Inhibition of YAP function overcomes BRAF inhibitor resistance in melanoma cancer stem cells." Oncotarget.2017 Nov 22;8(66):110257-110272. PMID:29299145
          9. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695
          10. Basu R, Baumgaertel N, et al. "Growth Hormone Receptor Knockdown
          Sensitizes Human Melanoma Cells to Chemotherapy by Attenuating Expression of ABC Drug Efflux Pumps. Horm Cancer." 2017 Jun;8(3):143-156. PMID:28293855
          11. Yuan He, Djoke Hendriks, et al. "Melanoma-directed activation of apoptosis using a novel bispecific antibody directed at MCSP and TRAIL receptor 2/Death Receptor 5." Journal of Investigative Dermatology,February 2016, volume 136, pages 541-4.

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