产品
编 号：F485557
分子式：C22H28ClN7O3S
分子量：506.02
分子式：C22H28ClN7O3S
分子量：506.02
产品类型
规格
价格
是否有货
50mg
640
In-stock
100mg
960
In-stock
结构图
CAS No: 863127-77-9
产品详情
生物活性：
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
体内研究：
Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels. Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%.Animal Model:Nude mice bearing K562 xenografts
Dosage:5 mg/kg and 50 mg/kg
Administration:Oral administration on a 5 day on and 2 day off schedule.
Result:Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model:Sprague-Dawley Rats
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral and i.v.
Result:Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
体外研究：
Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of Dasatinib monohydrate 相关抗体:
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
体内研究：
Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels. Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%.Animal Model:Nude mice bearing K562 xenografts
Dosage:5 mg/kg and 50 mg/kg
Administration:Oral administration on a 5 day on and 2 day off schedule.
Result:Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model:Sprague-Dawley Rats
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral and i.v.
Result:Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
体外研究：
Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of Dasatinib monohydrate 相关抗体:
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备