产品
编 号：F034640
分子式：C26H31BrN8O
分子量：551.48
分子式：C26H31BrN8O
分子量：551.48
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1095382-05-0
产品详情
生物活性：
CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
体内研究：
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.
体外研究：
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.
CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
体内研究：
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.
体外研究：
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.
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