CD532

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CD532 是一种有效的 Aurora A 激酶抑制剂，IC50 值为 45 nM。CD532 具有阻断 Aurora A 激酶活性和驱动 MYCN 降解的双重作用。CD532 还可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于癌症的研究。

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.

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.Cell Viability Assay Cell Line:SK-N-BE(2) and Kelly cells Concentration:1, 10, 100, 1000, 10000 nM Incubation Time:72 hours Result :Inhibited the cell viability of SK-N-BE(2) and Kelly cells, with EC50s of 223.2 nM and 146.7 nM, respectively.Cell Cycle Analysis Cell Line:SK-N-BE(2) cells Concentration:1 μM Incubation Time:4 hours Result:Resulted in a rapid and potent loss of S-phase and accumulation in both G0/G1 and G2.Western Blot Analysis Cell Line:SK-N-BE(2) cells Concentration:0.1, 0.25, 0.5, 1 μM Incubation Time:2, 4, 6, 24 hours Result:Causes dose-dependent and time-dependent loss of MYCN protein.

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.

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Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

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1639009-81-6

522.52

C26H25F3N8O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (478.45 mM; 超声助溶 )

N(C=1C=C(NN1)C2CCCC2)C3=NC(NC4=CC=C(NC(NC5=CC(C(F)(F)F)=CC=C5)=O)C=C4)=NC=C3

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(-20℃)

With Ice Pack

≥ 2 years