购物车
  • 全部删除
  • TargetMol
    您的购物车当前为空

Rebastinib

Rating icon 很棒
产品编号 T2640Cas号 1020172-07-9
别名 DCC-2036, DCC2036, DCC 2036

Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50分别为 0.8 nM 和 4 nM,还抑制 LYN、SRC、HCK、FGR、FLT3、KDR 和 Tie-2,对 c-Kit 的活性低。Rebastinib 对 Angiopoietin2-Tie2通路具有抑制作用。

Rebastinib
TargetMol

为众多的药物研发团队赋能,

让新药发现更简单!

Rebastinib

Rating icon 很棒
纯度: 99.84%
产品编号 T2640 别名 DCC-2036, DCC2036, DCC 2036Cas号 1020172-07-9

Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50分别为 0.8 nM 和 4 nM,还抑制 LYN、SRC、HCK、FGR、FLT3、KDR 和 Tie-2,对 c-Kit 的活性低。Rebastinib 对 Angiopoietin2-Tie2通路具有抑制作用。

规格价格库存数量
1 mg¥ 239现货
5 mg¥ 534现货
10 mg¥ 897现货
25 mg¥ 1,540现货
50 mg¥ 2,310现货
100 mg¥ 3,490现货
大包装 & 定制
加入购物车
实验操作小课堂
查看更多

"Rebastinib"的相关化合物库

选择批次:
纯度:99.84%
联系我们获取更多批次信息
TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性
产品描述
DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.
靶点活性
Abl-1 (WT):0.8 nM, Abl-1 (T315I):4 nM
体外活性
给在携带Ba/F3-BCR-ABL1T315I白血病细胞的小鼠移植瘤模型中,DCC-2036(100 mg/kg/day,p.o.)对BCR-ABL1信号具有明显抑制效果,并显著延长小鼠寿命.
体内活性
DCC-2036对野生型或突变型BCR-ABL1的Ba/F3细胞有抗增殖活性(IC50:2-150 nM)。此外,DCC-2036对Ph+细胞系K562增殖也有抑制作用(IC50:5.5 nM),并有效诱导表达BCR-ABL1的Ba/F3和K562细胞凋亡。 通过对CML细胞系的显著抑制(与非CML白血病细胞系相比),DCC-2036可选择性抑制BCR-ABL阳性细胞。DCC-2036对纯化的未磷酸化和磷酸化ABL1(IC50:0.8/2 nM)、未磷酸化和磷酸化突变型ABL1T315I(IC50:1.4/5 nM)及激活环突变ABL1H396P(IC50:4 nM)呈较强的非ATP竞争性抑制作用。DCC-2036还抑制SRC家族激酶SRC/LYN/FGR/HCK及受体 TKs KDR/FLT3/TIE2(IC50:34/29/38/40/4/2/6 nM)。
激酶实验
Assay of Abl1 kinase isoforms and determination of inhibitor potency: Activity of u-Abl1native is determined by following the production of ADP from the kinase reaction through coupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (measured as a decreased A340 nM) is continuously monitored spectrophotometrically. The final reaction mixture (100 μL, in a 384-well Corning plate) is prepared as follows: An Abl1 kinase/coupled assay components mixture is prepared containing u-Abl1 kinase (1 nM), Abltide (EAIYAAPFAKKK, 0.2 mM), MgCl2 (9 mM), pyruvate kinase (~ 4 units), lactate dehydrogenase (~ 0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28 mM) in 90 mM Tris containing 0.1 % octyl-glucoside and 1 % DMSO, pH 7.5. Separately, an inhibitor mixture is prepared containing DCC-2036 serially diluted 3-fold in DMSO followed by dilution into buffer composed of 180 mM Tris, pH 7.5, containing MgCl2 (18 mM) and 0.2 % octyl-glucoside. Fifty μL of the inhibitor mixture is mixed with 50 μL of the above Abl1 kinase/coupled assay components mixture, which is then incubated at 30 °C for 2 hours before 2 μL of 25 mM ATP (500 μM, final) is added to start the reaction. The reaction is recorded every 2 minutes for 2.5 hours at 30 °C on a Polarstar Optima or Synergy2 plate reader. Reaction rate (slope) is calculated using the 1 to 2 hour time frame with reader's software. Percent inhibition is obtained by comparison of reaction rate with that of a DMSO control. IC50 values are calculated from a series of percent inhibition values determined at a range of inhibitor concentrations using GraphPad Prism. The kinase assay for Abl1T315I, p-Abl1native or Abl1H396P is assayed the same as above except that 2.2 nM Abl1T315I, 1 nM p-Abl1 native or 1.3 nM Abl1H396P is used. The above assay format is also used for kinases other than Abl1 with the exception of TIE2, for which a fluorescence polarization/Transcreener format is used.The assay conditions are the same as described above except that PolyE4Y (final 1 mg/mL) is used as the substrate and one hour preincubation is used.
细胞实验
Ba/F3 cells or primary Ph+ leukemia cells are plated in triplicate in 96-well plates containing test compounds. After 72 hours, viable cells are quantified by Resazurin or MTT assay. Cells are diluted in medium to be added to each well of a 96-well tissue culture-treated plate. All cells are incubated overnight and maintained in a humidified atmosphere at 37 °C and 5% CO2. Cells are treated the following day. Serum-free medium is used during treatment with DCC-2036. MTT is used to assess the viability of cells following treatment. Aliquots of 20 mL of stock MTT solution are added to each well containing 200 mL of medium (10% final solution) and incubated with the cells for 2 hours. Following incubation the medium is removed and 200 mL of dimethylsulfoxide added to solubilize the formazan crystals. The absorbance is read on the plate reader at 550 and 690 nm. A subtraction analysis of the dual wavelength is performed (D550 to D690) to increase accuracy of the measuremen(Only for Reference)
别名DCC-2036, DCC2036, DCC 2036
化学信息
分子量553.59
分子式C30H28FN7O3
CAS No.1020172-07-9
SmilesCNC(=O)c1cc(Oc2ccc(NC(=O)Nc3cc(nn3-c3ccc4ncccc4c3)C(C)(C)C)c(F)c2)ccn1
密度1.32 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 13 mg/mL (23.5 mM)
DMSO: 5.53 mg/mL (10 mM), Sonication is recommended.
溶液配制表
1mg5mg10mg50mg
1 mM1.8064 mL9.0320 mL18.0639 mL90.3196 mL
5 mM0.3613 mL1.8064 mL3.6128 mL18.0639 mL
10 mM0.1806 mL0.9032 mL1.8064 mL9.0320 mL
1mg5mg10mg50mg
20 mM0.0903 mL0.4516 mL0.9032 mL4.5160 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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
%
%Tween 80
%ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

关键词

评论列表

4个月前
5.0
Rating icon 很棒

评论内容

Related Tags: buy Rebastinib | purchase Rebastinib | Rebastinib cost | order Rebastinib | Rebastinib chemical structure | Rebastinib in vivo | Rebastinib in vitro | Rebastinib formula | Rebastinib molecular weight