Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride 是一种具有口服活性的,ATP 竞争性的,双重 Src/Bcr-Abl 抑制剂,具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib hydrochloride hydrochloride 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib hydrochloride hydrochloride 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 328 | 现货 | ||
50 mg | ¥ 460 | 现货 | ||
100 mg | ¥ 587 | 现货 | ||
200 mg | ¥ 713 | 现货 | ||
500 mg | ¥ 1,198 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | Dasatinib hydrochloride (BMS-354825 HCl) (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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13.5 mg/mL (25.7 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9067 mL | 9.5334 mL | 19.0669 mL | 47.6672 mL |
5 mM | 0.3813 mL | 1.9067 mL | 3.8134 mL | 9.5334 mL | |
10 mM | 0.1907 mL | 0.9533 mL | 1.9067 mL | 4.7667 mL | |
20 mM | 0.0953 mL | 0.4767 mL | 0.9533 mL | 2.3834 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dasatinib hydrochloride 854001-07-3 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src c-Kit BMS-354825 HCl Dasatinib Hydrochloride Inhibitor inhibitor inhibit