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CCT137690, an aurora kinase inhibitor CCT137690, is a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays and exhibits anti-proliferative activity against a wide range of human solid tumour cell lines. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis. This is accompanied by p53/p21/BAX induction, thymidine kinase 1 (TK1) downregulation and PARP cleavage. Furthermore, CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression. Importantly, in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation, this compound significantly inhibits tumour growth. The potent preclinical activity of CCT137690 suggests that this inhibitor may benefit patients with MYCN amplified neuroblastoma. (source: Mol Cancer Ther. 2011 Nov;10(11):2115-23.).
CCT-137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively). CCT-137690 displays antiproliferative activity in a range of human tumor cell lines. Orally bioavailable.
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. Epub 2011 Sep 1. PubMed PMID: 21885865.
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
(Keyword; CAS#; MedKoo code#)
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