PLX8394

• CAT Number: I001508
• CAS Number: 1393466-87-9
• Molecular Formula: C25H21F3N6O3S
• Molecular Weight: 542.53
• Purity: ≥95%
• Target: B-RafV600E
• Solubility: DMSO: ≥ 39 mg/mL
• Storage: Store at -20°C
• IC50: ~5 nM
• IUPAC Name: (3R)-N-[3-[5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]-3-fluoropyrrolidine-1-sulfonamide
• InChI: InChI=1S/C25H21F3N6O3S/c26-16-5-6-34(12-16)38(36,37)33-20-4-3-19(27)21(22(20)28)23(35)18-11-32-25-17(18)7-14(8-31-25)15-9-29-24(30-10-15)13-1-2-13/h3-4,7-11,13,16,33H,1-2,5-6,12H2,(H,31,32)/t16-/m1/s1
• InChIKey: YYACLQUDUDXAPA-MRXNPFEDSA-N
• SMILES: C1CC1C2=NC=C(C=N2)C3=CN=C4C(=C3)C(=CN4)C(=O)C5=C(C=CC(=C5F)NS(=O)(=O)N6CCC(C6)F)F

PLX8394 (CAT: I001508) is a selective inhibitor of the BRAF kinase, a protein involved in cell signaling pathways related to cell growth and proliferation. Specifically, PLX8394 targets mutated forms of BRAF, such as BRAF V600E, which are commonly found in certain types of cancer, including melanoma. By inhibiting the activity of mutated BRAF, PLX8394 disrupts the signaling cascade that promotes tumor growth and survival. It has shown promise in preclinical studies and is being investigated as a potential targeted therapy for cancer treatment, particularly in patients with BRAF-mutant cancers. Clinical trials are ongoing to assess the safety and efficacy of PLX8394 in cancer patients.

Reference

[1]. Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-484.
[2]. Zhang C, et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015 Oct 22;526(7574):583-586.