PLX-4032

• CAT Number: A000179
• CAS Number: 918504-65-1
• Molecular Formula: C₂₃H₁₈ClF₂N₃O₃S
• Molecular Weight: 489.92
• Purity: ≥95%
• Synonyms: RO5185426
• Target: Autophagy
• Solubility: >24.5mg/mL in DMSO
• IUPAC Name: N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
• InChI: 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)
• InChIKey: GPXBXXGIAQBQNI-UHFFFAOYSA-N
• SMILES: CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)Cl)F

PLX-4032 (also known as Vemurafenib)（Cat No.:A000179）is a selective inhibitor of the BRAF V600E mutation, a common mutation found in various cancers, particularly melanoma. By targeting this mutated form of BRAF, PLX-4032 disrupts the MAPK/ERK signaling pathway, leading to reduced cell proliferation and increased apoptosis in cancer cells. It has been used in the treatment of melanoma with BRAF mutations, showing significant clinical efficacy. PLX-4032 is a critical tool in cancer research and drug development, particularly for exploring targeted therapies in BRAF-mutant tumors.

Reference

1: Pellowska M, Merk D, Schubert-Zsilavecz M. Advances in personalized medicine – medicinal chemistry and pharmacology of vemurafenib and ivacaftor. Pharmazie. 2013 Jul;68(7):484-91. Review. PubMed PMID: 23923627.
2: Banaszynski M, Kolesar JM. Vemurafenib and ipilimumab: new agents for metastatic melanoma. Am J Health Syst Pharm. 2013 Jul 15;70(14):1205-10. doi: 10.2146/ajhp120260. Review. PubMed PMID: 23820456.
3: Liszkay G. [Vemurafenib (Zelboraf) in the therapy of melanoma]. Magy Onkol. 2013 Jun;57(2):110-3. doi: MagyOnkol.2013.57.2.110. Epub 2013 May 14. Review. Hungarian. PubMed PMID: 23795356.
4: Shaw HM, Nathan PD. Vemurafenib in melanoma. Expert Rev Anticancer Ther. 2013 May;13(5):513-22. doi: 10.1586/era.13.24. Review. PubMed PMID: 23617343.
5: Gonzalez D, Fearfield L, Nathan P, Tanière P, Wallace A, Brown E, Harwood C, Marsden J, Whittaker S. BRAF mutation testing algorithm for vemurafenib treatment in melanoma: recommendations from an expert panel. Br J Dermatol. 2013 Apr;168(4):700-7. doi: 10.1111/bjd.12248. Review. PubMed PMID: 23360189.
6: Sharma A, Shah SR, Illum H, Dowell J. Vemurafenib: targeted inhibition of mutated BRAF for treatment of advanced melanoma and its potential in other malignancies. Drugs. 2012 Dec 3;72(17):2207-22. doi: 10.2165/11640870-000000000-00000. Review. PubMed PMID: 23116250.
7: Jordan EJ, Kelly CM. Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. Review. PubMed PMID: 23094782.
8: Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov. 2012 Nov;11(11):873-86. doi: 10.1038/nrd3847. Epub 2012 Oct 12. Review. PubMed PMID: 23060265.
9: Keating GM. Vemurafenib: in unresectable or metastatic melanoma. BioDrugs. 2012 Oct 1;26(5):325-34. doi: 10.2165/11209860-000000000-00000. Review. PubMed PMID: 22946753.
10: Boyd KP, Vincent B, Andea A, Conry RM, Hughey LC. Nonmalignant cutaneous findings associated with vemurafenib use in patients with metastatic melanoma. J Am Acad Dermatol. 2012 Dec;67(6):1375-9. doi: 10.1016/j.jaad.2012.06.045. Epub 2012 Aug 30. Review. PubMed PMID: 22940405.