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Dubermatinib

Dubermatinib

产品编号 T2005   CAS 1341200-45-0
别名: TP0903

Dubermatinib (TP0903) 是一种具有高效性和选择性的 Axl 受体酪氨酸激酶抑制剂,IC50值为27 nM。

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Dubermatinib Chemical Structure
Dubermatinib, CAS 1341200-45-0
规格 价格/CNY 货期 数量
1 mg ¥ 239 现货
2 mg ¥ 415 现货
5 mg ¥ 657 现货
10 mg ¥ 937 现货
25 mg ¥ 1,960 现货
50 mg ¥ 3,920 现货
100 mg ¥ 5,590 现货
500 mg ¥ 11,600 现货
产品目录号及名称: Dubermatinib (T2005)
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纯度: 98.92%
纯度: 98.76%
纯度: 98.65%
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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 Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.
靶点活性 Axl:27 nM
体外活性 In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. [1] In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis. [2]
体内活性 In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities. [4]
激酶实验 Axl Kinase activity assay: Test compounds are diluted to desired concentrations in kinase reaction buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT, and 0.01% v/v Tween-20) and are briefly incubated with Axl kinase. The Axl kinase used is recombinant human Axl kinase (catalytic domain, amino acids 473-894) with a histidine tag. The reaction is initiated by the addition of ATP and fluorescein-labeled poly-GT substrate (poly Glu:Tyr, 4:1 polymer). Concentration of the various components in the assay (10 μL reaction volume) are: 1% DMSO, 93 ng/mL Axl kinase, 20 μM ATP, and 200 nM fluorescein poly-GT substrate. Following addition of ATP and fluorescein poly-GT substrate, incubation is for 60 min at room temperature, the enzyme reaction is stopped by addition of 10 μL terbium-labeled anti-phosphotyrosine PY20 antibody in EDTA-containing buffer. Final concentration of EDTA and antibody after addition to the reaction is 10 mM and 2 nM, respectively. The terbium conjugated antibody generates a time-resolved FRET signal with the fluorescein molecule (bound to the poly-GT substrate) when the substrate is phosphorylated. After one hour incubation at room temperature, fluorescence is measured with excitation of 320 nm and dual emission of 495 and 520 nm on an EnVision microplate reader. Signal is expressed in -636996terms of a TR-FRET ratio (fluorescence intensity at 520 nm to 495 nm).
细胞实验 For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, TP-0903 is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader[1].
别名 TP0903
分子量 516.06
分子式 C24H30ClN7O2S
CAS No. 1341200-45-0

存储

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

溶解度

DMSO: Slightly soluble

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. Mollard A, et al. ACS Med Chem Lett. 2011, 2(12), 907-912. 2. Sinha S, et al. Clin Cancer Res. 2015, 21(9), 2115-2126.
Kinsenoside CAY10404 Apoptozole Cambinol Kaempferol Docetaxel HLCL-61 hydrochloride Pracinostat

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 抗癌药物库 酪氨酸激酶分子库 抗癌活性化合物库 激酶抑制剂库 抗乳腺癌化合物库 临床期小分子药物库 细胞凋亡化合物库 经典已知活性库 已知活性化合物库

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
g
给药体积
μL
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。
% DMSO
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% Tween 80
% ddH2O
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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

Dubermatinib 1341200-45-0 Apoptosis Tyrosine Kinase/Adaptors TAM Receptor Mer TP0903 TP-0903 TP 0903 inhibit Axl Inhibitor Tyro3 inhibitor

 

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