产品信息
抗原名称
Bcr-Abl
商品描述
Dasatinib hydrochloride is a potent and dual Abl/ Src inhibitor IC50 of ??1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM.
分子量
524.47
纯度
>98%
可溶性
DMSO: 15 mg/mL
In vitro(体外研究)
Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC50≤1.7 nM). Dasatinib (IC50: 0.8 nM) displays 325-fold greater potency compared with Imatinib against cells expressing wild-type Bcr-Abl in Ba/F3 cells.
In vivo(体内研究)
Daily treatment with Dasatinib (50 mg/kg) is initiated on day 10. Using this approach, a significant inhibition of BCPAP orthotopic tumor growth is observed 6 days after treatment (day 16, P=0.014), which is sustained through days 23 and 29 (P=0.0003), compared with vehicle-treated mice. Metabolism studies of Dasatinib (50 mg/kg) in rat suggested that Dasatinib is the major circulating component, whereas multiple metabolites contributed to the remaining 40-60% of the sample radioactivity at 4 h post dose.
背景
别名
BMS-354825 hydrochloride, Sprycel hydrochloride, BMS354825 hydrochloride, BMS 354825 hydrochloride
分子式
C22H27Cl2N7O2S
CAS号
854001-07-3
制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
参考图片
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