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Dasatinib

Dasatinib

产品编号 T1448   CAS 302962-49-8
别名: BMS-354825, 达沙替尼

Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂,抑制 SrcBcr-Abl (Ki=16/30 pM),具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性,用于治疗白血病和淋巴瘤等。

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Dasatinib Chemical Structure
Dasatinib, CAS 302962-49-8
规格 价格/CNY 货期 数量
10 mg ¥ 253 现货
50 mg ¥ 734 现货
100 mg ¥ 996 现货
200 mg ¥ 1,381 现货
500 mg ¥ 1,997 现货
1 mL * 10 mM (in DMSO) ¥ 152 现货
其他形式的 Dasatinib:
产品目录号及名称: Dasatinib (T1448)
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纯度: 99.89%
纯度: 99.86%
纯度: 99.62%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.
靶点活性 c-Kit (D816V):37 nM (cell free), Abl:0.6 nM (cell free), c-Kit wt:79 nM (cell free), Src:0.8 nM (cell free)
体外活性 方法:8 种甲状腺癌细胞用 Dasatinib (0.019-1.25 μmol/L) 处理 3 天,使用 SRB 方法检测细胞增殖。
结果:Dasatinib 对 C643、TPC1、BCPAP、SW1736、K1、8505C、HTh74、HTh7 细胞的 IC50 分别为 0.09、0.03、0.04、0.08、0.4、2.7、>5、1.6 μmol/L。[1]
方法:人肺癌细胞 NCI-H1975 和 NCI-H1650 用 Dasatinib (2.5-20 μM) 处理 48 h,使用 Flow Cytometry 检测细胞凋亡情况。
结果:Dasatinib 在 10 和 20 μM 下诱导 NCI-H1975 和 NCI-H1650 细胞凋亡。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Dasatinib (50 mg/kg in 80 mmol/L sodium citrate buffer, pH 3.0) 口服给药给携带人甲状腺癌肿瘤 BCPAP 或 8505C 的 athymic nude 小鼠,每周五天,持续二十天。
结果:Dasatinib 显著抑制 BCPAP 原位肿瘤,最终肿瘤体积抑制了 90% 以上。Dasatinib 治疗在任何时间点都没有显著抑制 8505C 来源的肿瘤的生长。[1]
方法:为研究对神经炎症的影响,将 Dasatinib (20 mg/kg in 4%DMSO+30%PEG+5%Tween 80) 腹腔注射或口服给药给 C57BL6/N 小鼠,每天一次给药四天,随后腹腔注射 LPS (10  mg/kg) 诱导体内神经炎症反应。
结果:腹腔注射和口服 Dasatinib 抑制 LPS 诱导的野生型小鼠脑中小胶质细胞/星形胶质细胞活化、促炎细胞因子水平和中性粒细胞滚动。[3]
激酶实验 Kinase assays using wild-type and mutant glutathione S-transferase (GST)–Abl fusion proteins (c-Abl amino acids 220-498) were done as described, with minor alterations. GST-Abl fusion proteins were released from glutathione-Sepharose beads before use; the concentration of ATP was 5 μmol/L. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins were treated with LAR tyrosine phosphatase according to the manufacturer's instructions. After 1-hour incubation at 30°C, LAR phosphatase was inactivated by addition of sodium vanadate (1 mmol/L). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase was routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations were 0 to 5,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The BMS-354825 concentration range was extended to 1,000 nmol/L for mutant T315I. These same inhibitor concentrations were used for the in vitro peptide substrate phosphorylation assays. The three inhibitors were tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase [1].
细胞实验 Ba/F3 cell lines were plated in triplicate and incubated with escalating concentrations of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90 determinations were 0 to 2,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The imatinib concentration range was extended to 6,400 nmol/L for mutants with IC50 >2,000 nmol/L. The BMS-354825 concentration range was extended to 200 nmol/L for mutant T315I [1].
动物实验 For in vivo studies, dasatinib (50 mg/kg) was prepared for daily oral gavage (5 d/wk) in 80 mmol/L sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice were randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice received dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment) [4].
别名 BMS-354825, 达沙替尼
分子量 488.01
分子式 C22H26ClN7O2S
CAS No. 302962-49-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 91 mg/mL (186.5 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0491 mL 10.2457 mL 20.4914 mL 51.2285 mL
5 mM 0.4098 mL 2.0491 mL 4.0983 mL 10.2457 mL
10 mM 0.2049 mL 1.0246 mL 2.0491 mL 5.1228 mL
20 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5614 mL
50 mM 0.041 mL 0.2049 mL 0.4098 mL 1.0246 mL
100 mM 0.0205 mL 0.1025 mL 0.2049 mL 0.5123 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91. 2. Zhang M, et al. Dasatinib Inhibits Lung Cancer Cell Growth and Patient Derived Tumor Growth in Mice by Targeting LIMK1. Front Cell Dev Biol. 2020 Dec 4;8:556532. 3. Ryu KY, et al. Dasatinib regulates LPS-induced microglial and astrocytic neuroinflammatory responses by inhibiting AKT/STAT3 signaling. J Neuroinflammation. 2019 Oct 26;16(1):190. 4. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91. 5. Shen Z, et al. Metabolite profiling of dasatinib dosed to Wistar Han rats using automated dried blood spot collection. J Pharm Biomed Anal. 2012 Aug-Sep;67-68:92-7. 6. Kan He, et al. Protein kinase inhibitors. Patent. US20180099960A1.

文献引用

1. Cai Z, Wu X, Song Z, et al.Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis.Cell Discovery.2023, 9(1): 104. 2. Yan H, Wu W, Hu Y, et al.Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis.Nature Communications.2023, 14(1): 2756. 3. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023 4. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866. 5. Wang T, Yang C, Li Z, et al.Flavonoid 4, 4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy.Redox Biology.2023: 103017. 6. Li F, Wang Z, Zheng D, et al.NK92 cells and peripheral blood NK cells respond oppositely upon dasatinib treatment.Immunology.2024
CHMFL-ABL-121 Radotinib AST 487 Olverembatinib dimesylate Pivanex NVP-BHG712 CpCDPK1/TgCDPK1-IN-1 Masitinib

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌上市药物库 抗癌药物库 神经退行性疾病化合物库 酪氨酸激酶分子库 抗COVID-19化合物库 造血毒性小分子库 抑制剂库 心血管毒性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
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给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

Dasatinib 302962-49-8 Angiogenesis Apoptosis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src c-Kit active antiproliferative CML antitumor breast Inhibitor prostate BMS354825 colon K562 BMS-354825 WiDr 达沙替尼 PC3 orally BMS 354825 inhibit inhibitor

 

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