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抑制剂/激活剂

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凋亡与自噬

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Dasatinib (BMS-354825)

Dasatinib (BMS-354825) 达沙替尼; BMS-354825

Dasatinib是一种新型有效的多靶点抑制剂，作用于Abl、Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM、0.8 nM 和 79 nM。Dasatinib 可诱导自噬和凋亡并具有抗肿瘤的活性。

货号：
TK0196
规格：

5mg

10mg

25mg

50mg

100mg
价格：
￥0.00

产品参数

CAS No.	302962-49-8
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.
分子式	C22H26ClN7O2S
分子量	488.01
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 250 mg/mL (512.28 mM; Need ultrasonic)
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%.
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 <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively. Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively.
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纯度及产品资料	98%

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