产品
编 号:F762387
分子式:C26H25F3N8O
分子量:522.52
产品类型
结构图
CAS No: 1639009-81-6
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产品详情
生物活性:
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer.
体内研究:
CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival in mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma.CD532 (60 mg/kg; i.p. for 2 days) decreases the level of MYCN protein in MYCN-amplified neuroblastoma xenografts.CD532 (20 mg/kg; i.p.) shows a serum half-life of ~1.5 hours and AUC0-24 of 27 μM?h in mice.Animal Model:Homozygous nu/nu mice with SHH-subtype MYCN-expressing medulloblastoma
Dosage:25 mg/kg
Administration:I.p. twice weekly for 3 weeks
Result:Decreased the level of MYCN protein and tumor volume and increases survival.
体外研究:
CD532 (1-10000 nM; 72 h) is cytotoxic in MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, with EC50s of 223.2 nM and 146.7 nM, respectively.CD532 (0.1-1 μM; 24 h) causes dose-dependent loss of MYCN protein in SK-N-BE(2) cells.CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells.