CCT241161

• CAT Number: I005896
• CAS Number: 1163719-91-2
• Molecular Formula: C28H27N7O3S
• Molecular Weight: 541.63
• Purity: ≥95%
• Synonyms: CCT241161; CCT-241161; CCT 241161.;1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-(methylthio)-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea
• Target: pan-RAF inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term ,or -20 °C for long term
• IUPAC Name: 1-(5-tert-butyl-2-phenylpyrazol-3-yl)-3-[2-methylsulfanyl-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea
• InChI: InChI=1S/C28H27N7O3S/c1-28(2,3)22-15-23(35(34-22)17-8-6-5-7-9-17)32-27(37)31-19-11-10-18(14-21(19)39-4)38-20-12-13-29-26-25(20)30-16-24(36)33-26/h5-16H,1-4H3,(H,29,33,36)(H2,31,32,37)
• InChIKey: DPMYVVGAYAPQNS-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=NN(C(=C1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C(=NC=C3)NC(=O)C=N4)SC)C5=CC=CC=C5

CCT241161 (Cat.No:I005896) is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT241161 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK–ERK, in vitro and in vivo. CCT241161 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.

Reference

1: Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M, Suijkerbuijk BM, Menard D, McLeary R, Johnson L, Fish L, Ejiama S, Sanchez-Laorden B, Hohloch J, Carragher N, Macleod K, Ashton G, Marusiak AA, Fusi A, Brognard J, Frame M, Lorigan P, Marais R, Springer C. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell. 2015 Jan 12;27(1):85-96. doi: 10.1016/j.ccell.2014.11.006. Epub 2014 Dec 11. PubMed PMID: 25500121; PubMed Central PMCID: PMC4297292.