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CCT137690

CCT137690 1095382-05-0
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Chemical Information
Product name:CCT137690 Purity:98% min
CAS NO:1095382-05-0 Solubility:10 mM in DMSO
Molecular Formula:C26H31BrN8O Package:Package according to customer requirements
Molecular Weight:551.481 Storage:Store at -20℃
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Remarks
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.
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
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