Encorafenib

• CAT Number: I006669
• CAS Number: 1269440-17-6 (LGX-818); 1269440-29-0 (R-isomer of LGX-818).
• Molecular Formula: C22H27ClFN7O4S
• Molecular Weight: 540.01
• Purity: ≥95%
• Target: RAF inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term

Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Reference

1:A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer. van Geel RMJM, Tabernero J, Elez E, Bendell JC, Spreafico A, Schuler M, Yoshino T, Delord JP, Yamada Y, Lolkema MP, Faris JE, Eskens FALM, Sharma S, Yaeger R, Lenz HJ, Wainberg ZA, Avsar E, Chatterjee A, Jaeger S, Tan E, Maharry K, Demuth T, Schellens JHM.Cancer Discov. 2017 Mar 31. doi: 10.1158/2159-8290.CD-16-0795. [Epub ahead of print] PMID: 28363909 2:Can binimetinib, encorafenib and masitinib be more efficacious than currently available mutation-based targeted therapies for melanoma treatment? Turner MC, Rossfeld K, Salama AK, Tyler D, Beasley G.Expert Opin Pharmacother. 2017 Apr;18(5):487-495. doi: 10.1080/14656566.2017.1299710. Epub 2017 Mar 22. Review. PMID: 28277830 3:Cutaneous toxicity of a new BRAF inhibitor, LGX818 (encorafenib). Pascual LL, Muruzàbal RS, Gigli ML, Bayona JI.Indian J Dermatol Venereol Leprol. 2017 Jan-Feb;83(1):102-104. doi: 10.4103/0378-6323.191130. No abstract available. PMID: 27679406 Free Article4:Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the B-Raf inhibitor encorafenib, the EGFR inhibitors afatinib, erlotinib and gefitinib and the O-desmethyl metabolites of erlotinib and gefitinib in human plasma. Sparidans RW, Rosing H, Rood JJ, Schellens JH, Beijnen JH.J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Oct 15;1033-1034:390-8. doi: 10.1016/j.jchromb.2016.09.012. Epub 2016 Sep 11. No abstract available. PMID: 27639128 5:Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells. Li Z, Jiang K, Zhu X, Lin G, Song F, Zhao Y, Piao Y, Liu J, Cheng W, Bi X, Gong P, Song Z, Meng S.Cancer Lett. 2016 Jan 28;370(2):332-44. doi: 10.1016/j.canlet.2015.11.015. Epub 2015 Nov 14. PMID: 26586345