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CCT 137690

CAS No. : 1095382-05-0

MCE 站：CCT 137690

产品活性：CCT 137690是有效的，有口服活性的极光激酶 (aurora) 抑制剂，对极光激酶A，B，C的 IC₅₀ 值分别为15，25 和19 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：Aurora Kinase  |  Apoptosis

In Vitro: CCT 137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI₅₀=0.30 μM) and A2780 ovarian cancer cell line (GI₅₀=0.14 μM). CCT 137690 inhibits in vitro phosphorylation of histone H3. CCT 137690 is a moderate inhibitor of the hERG ion-channel (IC₅₀=3.0 μM). 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.

In Vivo: CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity. CCT 137690 significantly inhibits tumour growth in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation.

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