755038-65-4

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755038-65-4

编号ABP000330 化学名称N-[反式-4-[4-(环丙基甲基)-1-哌嗪基]环己基]-4-[[(7R)-7-乙基-5,6,7,8-四氢-5-甲基-8-异丙基-6-氧代-2-蝶啶基]氨基]-3-甲氧基苯甲酰胺 英文名称 BI6727 (Volasertib)/ MDL: MFCD20926414 分子式C34H50N8O3 分子量618.822 纯度 >99%

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化学名称 : N-[反式-4-[4-(环丙基甲基)-1-哌嗪基]环己基]-4-[[(7R)-7-乙基-5,6,7,8-四氢-5-甲基-8-异丙基-6-氧代-2-蝶啶基]氨基]-3-甲氧基苯甲酰胺

CAS : 755038-65-4

英文名称: BI6727 (Volasertib)/

英文同义词: VOLASERTIB

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

BI 6727 is a highly potent Polo-like kinase inhibitor with an IC50 of 0 .87 nM BI 6727 has an EC50 of 11-37 nM on a panel of cancer cell lines and selective dihydropteridinone with distinct properties. BI 6727 has a pharmacokinetic profile favoring sustained exposure of tumor tissues with a high volume of distribution and a long terminal half-life in mice. BI 6727 has physicochemical and pharmacokinetic properties that allow in vivo testing of i.v. as well as oral formulations, adding flexibility to dosing schedules. BI 6727 shows marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer.

参考文献

[1] Rudolph D et al. Clin Cancer Res. 2009 May 1; 15(9):3094-102.

[2] Schöffski P. Oncologist. 2009 Jun; 14(6):559-70.