Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0623 (RG 7421) 是一种 ATP 竞争性的MEK1抑制剂,Ki 值为 0.13 nM。它对 A375 细胞中 BRAFV600E 的 EC50值为 7 nM,而对 HCT116 细胞中 KRAS (G13D)的 EC50值为 42 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 533 | 现货 | ||
2 mg | ¥ 776 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,890 | 现货 | ||
25 mg | ¥ 2,850 | 现货 | ||
50 mg | ¥ 3,650 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,160 | 现货 |
产品描述 | GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1. |
靶点活性 | MEK1:0.13 nM(ki) |
体外活性 | AMG 925 shows potent antiproliferation efficacy against U937, MOLM13 and Colo205 cells with IC50 of 52 nM, 19 nM and 55 nM, respectively, and induces cell apoptosis. AMG 925 also inhibits pSTAT5 in MOLM13 and pRb via FLT3 and CDK4 inhibition in Colo205 with IC50 of 0.005 and 0.023 μM, respectively. [1] |
体内活性 | In NCR nude mice bearing MOLM13 tumors, AMG 925 (150 mg/kg, p.o.) inhibits STAT5 phosphorylation, and causes 100% tumor growth inhibition (TGI). [1] In mice bearing Colo205 xenografts, AMG 925 (50 mg/kg, p.o.) inhibits RB phosphorylation, and causes 97% tumor growth inhibition (TGI). [2] |
激酶实验 | Kinase Assays: The inhibitory activity of FLT3 is determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) assay. An ULight-labeled synthetic peptide (ULight-JAK1, PerkinElmer, Waltham, MA) derived from human Janus kinase 1 (amino acids 1015–1027) is used as the phosphoacceptor substrate. The FLT3 assay is conducted in a 384-well white OptiPlate in a total volume of 20 μL. The reaction mixture contains 50 nM ULight-JAK1, 116 μM ATP (equal to Km), 0.5 nM FLT3, and serially diluted test compounds in a reaction buffer of 50 mM Hepes, pH 7.6, 1 mM EGTA, 10 mM MgCl2, 2 mM DTT, and 0.005% Tween 20. The reaction is allowed to proceed for 1 h at room temperature and stopped by adding 20 μL of 20 mM EDTA and 4 nM LANCE Eu-W1024 antiphospho-tyrosine antibody in LANCE detection buffer. The plates are incubated at room temperature for 2 h after addition of detection reagents and are then read on an Envision multimode reader. Fluorescence signals measured at 615 nm (8.5 nm bandwidth) and 665 nm (7.5 nm bandwidth) with a 60 μs delay after excitation at 320 nm (75 nm bandwidth). The signal ratio at 665/615 nm (APC/Eu) was used in all data analyses. For CDK4 and CDK6 kinase assays, Rb (amino acids 773–928), and histone H1 are used as substrate for CDK4/6 and CDK1/2, respectively. Assays are performed in 96-well filter plates with a final volume of 100 μL, containing 1 μg Rb, 25 ng CDK4/cyclin D1, 25 μM ATP, 1 μCi [r-33P]-ATP, and compound in kinase reaction buffer (20 mM Tris-HCl, pH 7.4, 10 mM magnesium chloride, 5 mM β-glycerophosphate, 1 mM dithiothreitol, and 0.1% bovine serum albumin). Plates with reaction mix are incubated at room temperature for 60 min, and reactions are terminated by addition of 200 μL of 20% trichloroacetic acid. Wells are washed with 200 μL of 10% trichloroacetic acid and left to dry at room temperature. The bottom of the plates is sealed with tape, and 100 μL of MicroScint-20 scintillation cocktail are added to each well.Plates are read on a TopCount to determine radioactive incorporation. IC50 values are calculated by nonlinear regression curve fitting using GraphPad Prism v5.01. |
细胞实验 | Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5 × 103 cells/well in a total volume of 160 μL. The plates are incubated overnight to allow cells to attach. Test compounds are serially diluted into the plate (20 μL/well), and 20 μL/0.1 μCi of [14C]-thymidine are added to each well. Isotope incorporation is determined using a β plate counter after a further 72 h. IC50 values are determined by nonlinear regression curve fitting using GraphPad Prism v5.01.(Only for Reference) |
别名 | G-868, GDC0623, RG 7421, MEK inhibitor 1 |
分子量 | 456.21 |
分子式 | C16H14FIN4O3 |
CAS No. | 1168091-68-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 5 mg/mL(11 mM)
DMSO: 91 mg/mL(198.82 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.192 mL | 10.9599 mL | 21.9197 mL | 54.7993 mL |
5 mM | 0.4384 mL | 2.192 mL | 4.3839 mL | 10.9599 mL | |
10 mM | 0.2192 mL | 1.096 mL | 2.192 mL | 5.4799 mL | |
DMSO | 20 mM | 0.1096 mL | 0.548 mL | 1.096 mL | 2.74 mL |
50 mM | 0.0438 mL | 0.2192 mL | 0.4384 mL | 1.096 mL | |
100 mM | 0.0219 mL | 0.1096 mL | 0.2192 mL | 0.548 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。
GDC-0623 1168091-68-6 Apoptosis MAPK MEK G-868 G 868 Mitogen-activated protein kinase kinase GDC 0623 GDC0623 inhibit Inhibitor MAP2K MAPKK MEK inhibitor1 G868 RG 7421 MEK inhibitor-1 RG-7421 RG7421 MEK inhibitor 1 inhibitor