Rebastinib NEW
| Price | $63 | $97 | $181 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: Rebastinib | CAS No.: 1020172-07-9 |
| Purity: 99.84% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | 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. |
| 細胞實驗 | 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) |
| 激酶實驗 | 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. |
| 體外活性 | In a xenograft mouse model bearing Ba/F3-BCR-ABL1T315I leukemia cells, DCC-2036 (100 mg/kg/day, p.o.) significantly inhibits BCR-ABL1 signaling and notably prolongs the lifespan of the mice. |
| 體內(nèi)活性 | DCC-2036 exhibits antiproliferative activity against Ba/F3 cells expressing either wild-type or mutant BCR-ABL1, with IC50 values ranging from 2 to 150 nM. It also inhibits the proliferation of the Ph+ cell line K562 (IC50: 5.5 nM) and effectively induces apoptosis in Ba/F3 and K562 cells expressing BCR-ABL1. Notably, DCC-2036 selectively inhibits BCR-ABL positive cells by significantly suppressing CML cell lines compared to non-CML leukemia cell lines. It demonstrates potent non-ATP-competitive inhibition against unphosphorylated and phosphorylated ABL1 (IC50: 0.8/2 nM), unphosphorylated and phosphorylated mutant ABL1T315I (IC50: 1.4/5 nM), and the activation loop mutant ABL1H396P (IC50: 4 nM). Additionally, DCC-2036 inhibits SRC family kinases SRC/LYN/FGR/HCK and receptor TKs KDR/FLT3/TIE2 (IC50: 34/29/38/40/4/2/6 nM). |
| 存儲條件 | 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. |
| 關(guān)鍵字 | CD135 | Apoptosis | inhibit | Bcr-Abl | Fms like tyrosine kinase 3 | Inhibitor | FLT3 | Src | Cluster of differentiation antigen 135 | Rebastinib |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 神經(jīng)退行性疾病化合物庫 | 激酶抑制劑庫 | 酪氨酸激酶分子庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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