名称 | CD532 |
描述 | CD532 is A highly potent Aurora A kinase inhibitor with an IC50 value of 45 nM. CD532 can block Aurora A kinase activity, drive MYCN degradation, and can directly interact with AURKA and induce global conformational transformation. CD532 can be used to study cancer. |
体外活性 | In MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, CD532 (1-10000 nM; 72 h) exhibits cytotoxicity with EC50s of 223.2 nM and 146.7 nM, respectively[1].
In SK-N-BE(2) cells, CD532 (0.1-1 μM; 24 h) causes a dose-dependent loss of MYCN protein[1].
Furthermore, CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells[1]. |
体内活性 | In mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma, CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival[1].
In MYCN-amplified neuroblastoma xenografts, CD532 (60 mg/kg; i.p. for 2 days) reduces the level of MYCN protein[1].
CD532 (20 mg/kg; i.p.) in mice exhibits a serum half-life of ~1.5 hours and an AUC0-24 of 27 μM•h[1]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 200 mg/mL (382.76 mM), Sonication is recommended.
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关键字 | CD532 | CD-532 | CD 532 | 1[4({4[(5cyclopentyl1Hpyrazol3yl)imino]1,4dihydropyrimidin2yl}amino)phenyl]3[3(trifluoromethyl)phenyl]urea | 1 [4 ({4 [(5 cyclopentyl 1H pyrazol 3 yl)imino] 1,4 dihydropyrimidin 2 yl}amino)phenyl] 3 [3 (trifluoromethyl)phenyl]urea |
相关产品 | Palmatine chloride | MK-8745 | SC-514 | MBM-55S | SP600125 | KW-2449 | Palmatine | Alisertib | TAK-901 | TCS7010 |
相关库 | 经典已知活性库 | 表观遗传库 | 激酶抑制剂库 | 抑制剂库 | 已知活性化合物库 |