Vemurafenib

• Description :

  Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

• Product Name Alternative :

  PLX4032; RG7204; RO5185426

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Autophagy; Raf

• Type :

  Reference compound

• Related Pathways :

  Autophagy; MAPK/ERK Pathway

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Vemurafenib.html

• Purity :

  99.85

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  FC1=CC=C(C(F)=C1C(C2=CNC3=NC=C(C=C32)C4=CC=C(C=C4)Cl)=O)NS(CCC)(=O)=O

• Molecular Formula :

  C23H18ClF2N3O3S

• Molecular Weight :

  489.92

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467 (7315), 596-599.|[2]Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70 (13), 5518-5527.|[3]Prahallad A, et al. Unresponsiveness of colon cancer to BRAF (V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483 (7387), 100-103.|[4]Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6 (4) :361-5.|[5]Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102 (2) :634-643.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  B-Raf; C-Raf

• CAS Number :

  [918504-65-1]