Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DDR1-IN-1 是一种特异性的 DDR1 受体酪氨酸激酶抑制剂,选择性是 DDR2 的 3 倍左右。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 333 | 现货 | ||
2 mg | ¥ 482 | 现货 | ||
5 mg | ¥ 793 | 现货 | ||
10 mg | ¥ 1,260 | 现货 | ||
25 mg | ¥ 2,750 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,830 | 现货 | ||
500 mg | ¥ 11,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 963 | 现货 |
产品描述 | DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2. |
靶点活性 | DDR1:105 nM |
体外活性 | In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1. [1] |
激酶实验 | General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513). |
细胞实验 | Cells are plated in triplicate at a density of 3000 cells per well in 96-well plates and 1500 cells per well in 384-well plates. Compounds of various concentrations are added into plates for 48 hours. Cell viability is determined using the CellTiter-Glo and CCK-8. Both assays are performed according to the manufacturer's instructions. For CellTiter-Glo assay, luminescence is determined in a multi-label reader. For CCK-8 assay, absorbance is measured in a microplate reader at 450 nM. Data are normalized to control group (DMSO) and represented by the mean of at least two independent measurement with standard error <20%. GI50 were calculated using Prism 5.0.(Only for Reference) |
分子量 | 552.59 |
分子式 | C30H31F3N4O3 |
CAS No. | 1449685-96-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (168.3 mM)
Ethanol: 4 mg/mL(7.23 mM), Heating is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.8097 mL | 9.0483 mL | 18.0966 mL | 45.2415 mL |
5 mM | 0.3619 mL | 1.8097 mL | 3.6193 mL | 9.0483 mL | |
DMSO | 10 mM | 0.181 mL | 0.9048 mL | 1.8097 mL | 4.5241 mL |
20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2621 mL | |
50 mM | 0.0362 mL | 0.181 mL | 0.3619 mL | 0.9048 mL | |
100 mM | 0.0181 mL | 0.0905 mL | 0.181 mL | 0.4524 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。
Ddr1-In-1 1449685-96-4 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) Discoidin Domain Receptor inhibit Ddr-1-In-1 Inhibitor Ddr1 In 1 Ddr1In1 inhibitor