Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNF-5837 是一种选择性的,有效的,口服生物利用的泛TRK 抑制剂,在 Ba/F3 细胞中显示出抗增殖作用 (对Tel-TrkC,Tel-TrkB 和Tel-TrkA 的IC50值分别为 7 nM,9 nM 和 11 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 258 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,230 | 现货 | ||
50 mg | ¥ 1,990 | 现货 | ||
100 mg | ¥ 3,290 | 现货 | ||
200 mg | ¥ 4,290 | 现货 | ||
500 mg | ¥ 6,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 488 | 现货 |
产品描述 | GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM). |
靶点活性 | TrkA:8 nM, TrkB:12 nM |
体外活性 | In Ba/F3 cells overexpressing the constitutively active Tel-TRKC fusion, GNF-5837 shows potent anti-Trk activity and potent antiproliferation activity with IC50 of 0.042 μM. [1] |
体内活性 | In both male Balb/c mice and Sprague–Dawley rats, GNF-5837 has the low drug clearance, and moderate biovailability. In mice bearing Rie xenografts expressing TrkA and NGF, GNF-5837 (100 mg/kg/d p.o.) significantly inhibits tumor growth. [1] |
激酶实验 | Inhibition of biochemical TrkA,TrkB and TrkC: TrkA and TrkC biochemical assays are carried out by HTRF method.The reaction mixtures contains 1 μM peptide substrate,1 μM ATP,and either 1.8 nM TrkA or 34 nM TrkC in the reaction buffer (50 mM HEPES pH 7.1,10 mM MgCl2,2 mM MnCl2,0.01% BSA,2.5 mM DTT and 0.1 mM Na3VO4) at a final volume of 10 μL.All reactions are carried out at room temperature in white ProxiPlate? 384-well Plus plates and are quenched with 5 μL of 0.2 mM EDTA at 60 min.Five μL of the detection reagents (2.5 ng PT66K and 0.05 μg SAXL per well) are added,the plates are incubated at room temperature for 1 h and then read in EnVision reader.Compounds are diluted into assay mixture (final DMSO 0.5%),and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions.TrkB biochemical assay is carried out by caliper microfluidic method.The reaction mixtures contained 1 μM peptide substrate,10 μM ATP,and 2 nM TrkB in a reaction buffer containing 100 mM HEPES,pH 7.5,5 mM MgCl2,0.01% Triton X-100,0.1% BSA,1 mM DTT,10 μΜNa3VO4,and 10 μΜBeta-Glycerophosphate.The reactions are carried out at room temperature for 3 hrs,and the products are determined by Caliper EZ-reader.Compounds are diluted into assay mixture (final DMSO 1%),and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions. |
细胞实验 | Compounds are tested for their ability to inhibit the proliferation of wt Ba/F3 cells and Ba/F3 cells transformed with constitutively expressed luciferase reporter and BCR-ABL or Tel-KDR or other Tel fusion kinases. Parental Ba/F3 cells are maintained in media containing recombinant mouse IL3 and the kinase transformed Ba/F3 cells are maintained in media without IL-3. 7.5 nL of compounds are spotted to each well of 1536-well assay plates by Liquid handling System Echo 555 (Labcyte). 700 cells are then plated into each well of the assay plates in 7 μL culture media per well and compounds are tested at 0.17 nM to 10 uM in 3-fold serial dilutions. The cells were then incubated for 48 hours at 37 °C. 3 μL of Bright-Glo® is added to each well and the plates are read using ViewLux. (Only for Reference) |
别名 | GNF 5837 |
分子量 | 535.49 |
分子式 | C28H21F4N5O2 |
CAS No. | 1033769-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 5.4 mg/mL (10 mM)
DMSO: 53.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.8674 mL | 9.3372 mL | 18.6745 mL | 46.6862 mL |
5 mM | 0.3735 mL | 1.8674 mL | 3.7349 mL | 9.3372 mL | |
10 mM | 0.1867 mL | 0.9337 mL | 1.8674 mL | 4.6686 mL | |
DMSO | 20 mM | 0.0934 mL | 0.4669 mL | 0.9337 mL | 2.3343 mL |
50 mM | 0.0373 mL | 0.1867 mL | 0.3735 mL | 0.9337 mL | |
100 mM | 0.0187 mL | 0.0934 mL | 0.1867 mL | 0.4669 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
GNF-5837 1033769-28-6 Angiogenesis Tyrosine Kinase/Adaptors Trk receptor PDGFR c-Kit Tropomyosin related kinase receptor Trk Receptor GNF 5837 inhibit Inhibitor GNF5837 inhibitor