GSK-2118436 mesylate

• CAT Number: I000712
• CAS Number: 1195768-06-9
• Molecular Formula: C₂₄H₂₄F₃N₅O₅S₃
• Molecular Weight: 615.67
• Purity: ≥95%
• Synonyms: N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide;methanesulfonic acid
• Target: Raf
• Solubility: DMSO: ≥ 36 mg/mL
• Storage: Store at -20°C
• IC50: 3.2/0.8/5.0 nM (B-Raf/B-RafV600E/ c-Raf) [1]
• InChI: InChI=1S/C23H20F3N5O2S2.CH4O3S/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25;1-5(2,3)4/h4-11,31H,1-3H3,(H2,27,28,29);1H3,(H,2,3,4)
• InChIKey: YKGMKSIHIVVYKY-UHFFFAOYSA-N
• SMILES: O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C)(C)C)=N3)=C2F)=O.CS(O)(=O)=O

GSK-2118436 mesylate(Cat No.: I000712), also known as Dabrafenib mesylate, is a potent and selective inhibitor of the BRAF V600E mutation, a key driver in several cancers, including melanoma, non-small cell lung cancer (NSCLC), and thyroid cancer. By blocking aberrant BRAF signaling, it reduces tumor cell proliferation and survival. It is often used in combination therapies, particularly with MEK inhibitors, to prevent resistance. GSK-2118436 mesylate plays a critical role in targeted cancer therapy, offering improved outcomes for patients with BRAF-mutant tumors.

Reference

[1]. Sylvie Laquerre, et al. Abstract B88: A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation. Molecular Cancer Therapeutics: December 2009; Volume 8, Issue 12, Supplement 1
[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20.
[3]. Long GV, et al. Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial. Lancet Oncol. 2012 Nov;13(11):1087-95.
[4]. Falchook GS, et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet. 2012 May 19;379(9829):1893-901.