Dasatinib hydrochloride
作者：齐岳
发布时间：2023-08-23
09:17:19
点击数：
产品名称：Dasatinib hydrochloride
产品描述：
| 产品描述 | Dasatinib hydrochloride (BMS-354825) hydrochloride 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 hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy. |
| 靶点活性 | c-Kit (D816V):37 nM, Abl:0.6 nM, c-Kit (wt):79 nM, Src:0.8 nM |
| 体外活性 | Dasatinib hydrochloride 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 hydrochloride 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[1]. |
| 体内活性 | Dasatinib hydrochloride (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 hydrochloride (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib hydrochloride (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%[1]. |
| 别名 | BMS-354825 HCl |
| 分子量 | 524.47 |
| 分子式 | C22H27Cl2N7O2S |
| CAS No. | 854001-07-3 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 13.5mg/mL (25.7mM),Need ultrasonic and warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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