化合物 DCC-2036|T2640|TargetMol

Rebastinib
1020172-07-9

￥239 1mg 起订

￥534 5mg 起订

￥897 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 DCC-2036

英文名称：: Rebastinib

CAS号：: 1020172-07-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.84%

产品类别：: 抑制剂

货号：: T2640

Product Introduction

Bioactivity

名称	Rebastinib
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.
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)
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.
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）。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 13 mg/mL (23.5 mM) DMSO : 5.53 mg/mL (10 mM), Sonication is recommended.
关键字	CD135 \| Apoptosis \| inhibit \| Bcr-Abl \| Fms like tyrosine kinase 3 \| Inhibitor \| FLT3 \| Src \| Cluster of differentiation antigen 135 \| Rebastinib
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DCC2036|||DCC 2036|||DCC-2036|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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