CCT-137690

• CAT Number: I000402
• CAS Number: 1095382-05-0
• Molecular Formula: C₂₆H₃₁BrN₈O
• Molecular Weight: 551.48
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO 100 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 15 nM (Aurora A); 25 nM (Aurora B); 19 nM (Aurora C)
• IUPAC Name: 3-[[4-[6-bromo-2-[4-(4-methylpiperazin-1-yl)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]methyl]-5-methyl-1,2-oxazole
• InChI: InChI=1S/C26H31BrN8O/c1-18-15-20(31-36-18)17-33-9-13-35(14-10-33)24-22(27)16-28-26-23(24)29-25(30-26)19-3-5-21(6-4-19)34-11-7-32(2)8-12-34/h3-6,15-16H,7-14,17H2,1-2H3,(H,28,29,30)
• InChIKey: GFLQCBTXTRCREJ-UHFFFAOYSA-N
• SMILES: CC1=CC(=NO1)CN2CCN(CC2)C3=C4C(=NC=C3Br)N=C(N4)C5=CC=C(C=C5)N6CCN(CC6)C

CCT-137690 (Cat.No:I000402) is a selective and orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, including BRD2, BRD3, and BRD4. It has shown potent antiproliferative activity in a variety of cancer cell lines and demonstrated efficacy in several preclinical tumor models. Additionally, CCT-137690 has been found to inhibit the expression of key proinflammatory cytokines, suggesting potential therapeutic applications in inflammatory diseases.

Reference

[1]. Faisal A, Vaughan L, Bavetsias V, Sun C, Atrash B, Avery S, Jamin Y, Robinson SP, Workman P, Blagg J, Raynaud FI, Eccles SA, Chesler L, Linardopoulos S. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23.
[2]. Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28.
[3]. Moore AS, Faisal A, de Castro DG, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S. Selective FLT3 inhibition of FLT3-ITD(+) acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52.