产品
编 号：F311605
分子式：C22H26ClN7O2S
分子量：488.01
分子式：C22H26ClN7O2S
分子量：488.01
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
187
In-stock
10mg
280
In-stock
50mg
704
In-stock
100mg
960
In-stock
200mg
1320
In-stock
500mg
1920
In-stock
结构图
CAS No: 302962-49-8
产品详情
生物活性：
Dasatinib (BMS-354825) 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 inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
体内研究：
Dasatinib (5 mg/kg 和 50 mg/kg，qd×10d，5 on-2 off) 在慢性粒细胞白血病 (CML) 的 K562 异种移植模型中具有有效的抗肿瘤活性和高安全边际，表明肿瘤完全消退且低多剂量水平的毒性。 Dasatinib (10 mg/kg) 的药代动力学特征适合继续推进体内药效研究。Dasatinib (10 mg/kg) 在静脉注射和口服时表现出良好的半衰期 (t1/2s)，分别为 3.3 和 3.1 小时。本研究口服生物利用度 (Fpo) 为 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 对 Bcr-Abl、Src、Lck、Yes、c-Kit、PDGFRβ、p38、Her1、Her2、FGFR-1 和 MEK 具有显著活性，IC50Dasatinib 相关抗体:
Dasatinib (BMS-354825) 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 inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
体内研究：
Dasatinib (5 mg/kg 和 50 mg/kg，qd×10d，5 on-2 off) 在慢性粒细胞白血病 (CML) 的 K562 异种移植模型中具有有效的抗肿瘤活性和高安全边际，表明肿瘤完全消退且低多剂量水平的毒性。 Dasatinib (10 mg/kg) 的药代动力学特征适合继续推进体内药效研究。Dasatinib (10 mg/kg) 在静脉注射和口服时表现出良好的半衰期 (t1/2s)，分别为 3.3 和 3.1 小时。本研究口服生物利用度 (Fpo) 为 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 对 Bcr-Abl、Src、Lck、Yes、c-Kit、PDGFRβ、p38、Her1、Her2、FGFR-1 和 MEK 具有显著活性，IC50Dasatinib 相关抗体:
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