Bioactivity | TAK-901 hydrochloride is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively[1]. |
Invitro | TAK-901 对 Aurora B 展示了时间依赖性、紧密结合的抑制作用,但对Aurora A没有这种作用[1]。TAK-901 在 PC3 细胞中以剂量依赖性方式抑制组蛋白 H3 的磷酸化,EC50 值为 0.16 μM[1]。TAK-901 是 P-糖蛋白(PgP) 药物外排泵的底物,如在子宫肉瘤 MES-SA 细胞中EC50从38 nM下降到在高表达PgP的耐药MES-SA/Dx5细胞中超过 50 μM所示[1]。Cell line A2780 |
In Vivo | TAK-901 (在A2780和AML MV4-11裸鼠异种移植模型中) 分别以 30 和 40 mg/kg/注射的剂量可抑制肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 934542-50-4 |
Formula | C28H33ClN4O3S |
Molar Mass | 541.10 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Farrell P, et al. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol Cancer Ther. 2013 Apr;12(4):460-70. |