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Rebastinib

Rebastinib

产品编号 T2640   CAS 1020172-07-9
别名: DCC2036, DCC 2036, 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、SRCHCK、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。

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Rebastinib Chemical Structure
Rebastinib, CAS 1020172-07-9
规格 价格/CNY 货期 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
1 mL * 10 mM (in DMSO) ¥ 653 现货
产品目录号及名称: Rebastinib (T2640)
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纯度: 99.84%
纯度: 99.53%
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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 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 Abl1(WT):0.8 nM, Abl1(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 DCC2036, DCC 2036, DCC-2036
分子量 553.59
分子式 C30H28FN7O3
CAS No. 1020172-07-9

存储

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

溶解度

Ethanol: 13 mg/mL (23.5 mM)

DMSO: 103 mg/mL (186.1 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.8064 mL 9.032 mL 18.0639 mL 45.1598 mL
5 mM 0.3613 mL 1.8064 mL 3.6128 mL 9.032 mL
10 mM 0.1806 mL 0.9032 mL 1.8064 mL 4.516 mL
20 mM 0.0903 mL 0.4516 mL 0.9032 mL 2.258 mL
DMSO 50 mM 0.0361 mL 0.1806 mL 0.3613 mL 0.9032 mL
100 mM 0.0181 mL 0.0903 mL 0.1806 mL 0.4516 mL

计算器

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分子量计算器
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参考文献

1. Chan WW, et al. Cancer Cell. 2011, 19(4), 556-568. 2. Gillen J, Richardson D, Moore K. Angiopoietin-1 and Angiopoietin-2 Inhibitors: Clinical Development. Curr Oncol Rep. 2019 Feb 26;21(3):22.

文献引用

1. 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.
Sunitinib ATH686 GTP-14564 Sorafenib tosylate 3-Hydroxy Midostaurin KG5 UNC2025 BPR1J-097 hydrochloride (1327167-19-0(free base))

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 神经退行性疾病化合物库 酪氨酸激酶分子库 抗癌活性化合物库 抑制剂库 细胞骨架化合物库 细胞重编程化合物库 抗癌化合物库 ReFRAME 相关化合物库

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
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g
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

Rebastinib 1020172-07-9 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FLT Bcr-Abl Src CD135 inhibit Fms like tyrosine kinase 3 DCC2036 DCC 2036 DCC-2036 Inhibitor FLT3 Cluster of differentiation antigen 135 inhibitor

 

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