Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zoligratinib (CH5183284) 是一种口服具有活力的,选择性的FGFR 抑制剂,能够抑制FGFR1 (IC50:9.3 nM),FGFR2 (IC50:7.6 nM),FGFR3 (IC50:22 nM),FGFR4 (IC50:290 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 185 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,570 | 现货 | ||
50 mg | ¥ 2,570 | 现货 | ||
100 mg | ¥ 3,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), respectively. |
靶点活性 | FGFR4:290 nM, FGFR3:22 nM, FGFR1:9.3 nM, FGFR2:7.6 nM |
体外活性 | In the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 cell lines,CH5183284(100 to 300 nM) prevents autophosphorylation of FGFR1, FGFR2, and FGFR3. |
激酶实验 | Protein kinase assay: The inhibitory activity of CH5183284/Debio 1347 against FGFR1 is evaluated using a radiometric filter assay by measuring the incorporation of 33Pi with a microplate scintillation counter. The phosphorylation activities of LCK, EGFR, KIT, MET, SRC, BRK, FGFR2, Flt3, LTK, INSR, YES, ABL, EPHA2, ZAP70, Fyn, IGF1R, KDR, and PDGFR on substrate peptides are determined by homogeneous time-resolved fluorescence assay with LANCE Eu-W1024 labeled anti-phosphotyrosine PT66 antibody according to standard methods. Time-resolved fluorescence is measured with an EnVision HTS microplate reader. The activities of Aurora A, Akt1/PKBα, PKA, Cdk1/cyclin B, Cdk2/cyclin A, PKCα, PKCβ1 and PKCβ2 on substrate peptides are determined by IMAP FP Screening Express Progressive Binding System. Fluorescence polarization is measured with an EnVision HTS microplate reader. |
细胞实验 | The cell lines are added to the wells of 96-well plates containing 0.076 to 10,000 nM CH5183284/Debio 1347 and incubated at 37°C. After 4 days of incubation, Cell Counting Kit-8 solution is added and, after incubation for several more hours, absorbance at 450 nm is measured with the iMark Microplate-Reader. The antiproliferative activity is calculated using the formula (1 ? T/C) × 100 (%), where T and C represent absorbance at 450 nm of the cells treated with drugs (T) and that of untreated control cells (C). The IC50 values are calculated using Microsoft Excel 2007.(Only for Reference) |
别名 | FF284, CH5183284, Debio 1347 |
分子量 | 356.38 |
分子式 | C20H16N6O |
CAS No. | 1265229-25-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 1 mg/mL (2.8 mM), Heating is recommended.
DMSO: 66 mg/mL (185.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.806 mL | 14.03 mL | 28.0599 mL | 70.1498 mL |
DMSO | 5 mM | 0.5612 mL | 2.806 mL | 5.612 mL | 14.03 mL |
10 mM | 0.2806 mL | 1.403 mL | 2.806 mL | 7.015 mL | |
20 mM | 0.1403 mL | 0.7015 mL | 1.403 mL | 3.5075 mL | |
50 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.403 mL | |
100 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 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。
Zoligratinib 1265229-25-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR Debio1347 Fibroblast growth factor receptor CH 5183284 FF-284 FF284 Inhibitor CH5183284 Debio-1347 inhibit CH-5183284 Debio 1347 FF 284 inhibitor