Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1838705A 是一种高效的、可逆的IGF-IR (IC50:2.0 nM) 和胰岛素受体 (IC50:1.6 nM)抑制剂,也可抑制ALK (IC50:0.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 281 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,720 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 875 | 现货 |
产品描述 | GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases. |
靶点活性 | ALK:0.5 nM, IGF-1R:2 nM, Insulin Receptor:1.6 nM |
体外活性 | 在负荷COLO 205肿瘤的小鼠体内,GSK1838705A(30 mg/kg)可抑制80%的肿瘤生长.此外,在负荷HT29异种移植物或BxPC3异种移植物的小鼠体内,GSK1838705A也具有抗肿瘤作用.在负荷NIH-3T3/LISN肿瘤的小鼠体内,GSK1838705A(60 mg/kg,p.o.)抑制77%肿瘤生长,且体重无明显损失.在小鼠体内,通过抑制IR信号,GSK1838705A(60 mg/kg)可使血糖水平短暂增加2倍.GSK1838705A(60 mg/kg)抑制已建立的Karpas-299异种移植物的生长(93%),但不影响大鼠体重. |
体内活性 | GSK1838705A可有效抑制细胞中配体诱导的IGF-1R(IC50:85 nM)和IR(IC50:79 nM)磷酸化。GSK1838705A对一系列衍生自固体和血液肿瘤的细胞系,比如L-82/SUP-M2/SK-ES/MCF-7(EC50:24/28/141/203 nM)细胞均有显著抗增殖作用。GSK1838705A可使MCF-7 和NCl-H929细胞在细胞周期的G1 (2N)期积累。GSK1838705A对ALK也有抑制效果(Ki:0.35 nM),还抑制核仁磷酸蛋白(NPM)-ALK融合细胞的增殖(EC50:24-88 nM)。GSK1838705A对Karpas-299和SR-786细胞中的NPM-ALK磷酸化有显著抑制作用,但对STAT3磷酸化效果一般。 |
激酶实验 | Kinase Assays: Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determinations of IC50s by a homogeneous time-resolved fluorescence assay. A filter binding assay is used for appKi determinations using activated IGF-1R and IR kinases. Expanded kinase-selectivity profiling of GSK1838705A is carried out by screening the compound in the KinaseProfiler panel. |
细胞实验 | Cells are seeded in 96-well dishes, incubated overnight at 37 °C, and treated with DMSO or GSK1838705A for 72 hours. For the NIH-3T3/LISN proliferation assays, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 hours. The medium is replaced with serum-free medium and the cells are treated with GSK1838705A for 2 hour. Cells are incubated for 72 hours after addition of IGF-I (30 ng/mL). Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50s are determined from cytotoxicity curves using a four-parameter curve fit software package (XLfit4(Only for Reference) |
分子量 | 532.57 |
分子式 | C27H29FN8O3 |
CAS No. | 1116235-97-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 53.3 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8777 mL | 9.3884 mL | 18.7769 mL | 46.9422 mL |
5 mM | 0.3755 mL | 1.8777 mL | 3.7554 mL | 9.3884 mL | |
10 mM | 0.1878 mL | 0.9388 mL | 1.8777 mL | 4.6942 mL | |
20 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3471 mL | |
50 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 mL | |
100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4694 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。
GSK1838705A 1116235-97-2 Angiogenesis MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors S6 Kinase ALK IGF-1R JNK CD246 Anaplastic lymphoma kinase inhibit Cluster of differentiation 246 Anaplastic lymphoma kinase (ALK) ALK tyrosine kinase receptor GSK-1838705A Inhibitor Insulin Receptor inhibitor