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GSK1904529A

GSK1904529A

产品编号 T6003   CAS 1089283-49-7
别名: GSK 4529

GSK1904529A (GSK 4529) 是一种选择性,具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体和胰岛素受体抑制剂,IC50值分别为 27 和 25 nM。它具有抗肿瘤活性。

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GSK1904529A Chemical Structure
GSK1904529A, CAS 1089283-49-7
规格 价格/CNY 货期 数量
1 mg ¥ 296 现货
5 mg ¥ 698 现货
10 mg ¥ 1,120 现货
25 mg ¥ 1,880 现货
50 mg ¥ 2,870 现货
1 mL * 10 mM (in DMSO) ¥ 1,050 现货
产品目录号及名称: GSK1904529A (T6003)
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选择批次  
纯度: 98.89%
纯度: 98.66%
纯度: 98.2%
纯度: 98.07%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
靶点活性 IGF-1R:27 nM, Insulin Receptor:25 nM
体外活性 GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentrations above 0.01 μM, followed by blocking downstream signaling (AKT, IRS-1, and ERK). GSK1904529A potently inhibits NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES RD-ES cells with IC50 of 60 nM, 35 nM, 43 nM, 61 nM and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines including NCI-H929, MOLP-8, LP-1 and KMS-12-BM etc. GSK1904529A induces cell cycle arrest at the G1 phase in cell lines COLO 205, MCF-7, and NCI-H929, which are sensitive to GK1904529A. [1]
体内活性 GSK1904529A indicates 98% tumor growth inhibition in NIH-3T3/LISN tumor-bearing mice at a dose of 30 mg/kg (orally, twice-daily) and 75% in COLO 205 xenografts mice (once daily). Among HT29 and BxPC3 xenografts, GSK1904529A produces moderate tumor growth inhibition with no side effects at a dose of 30 mg/kg. Meanwhile, GSK1904529A shows minimal effects on blood glucose levels. GSK1904529A (~3.5 μM in blood) completely inhibits IGF-1R phosphorylation. GSK1904529A has been implicated in treatment of various IGF-1R-dependent tumors including prostate, colon, breast, pancreatic, ovarian, and sarcomas. [1]
激酶实验 Kinase assays: GSK1904529A is dissolved in DMSO as stock solution at 10 mM. 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 determination of IC50. Kinases are activated by preincubating the enzyme (2.7 μM final concentration) in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mg/mL bovine serum albumin, and 2 mM ATP. GSK1904529A is diluted in DMSO and dispensed into the assay plates (100 nL/well). Kinase reactions contained (in 10 μL) 50 mM HEPES (pH 7.5), 3 mM DTT, 0.1 mg/mL bovine serum albumin, 1 mM CHAPS, 10 mM MgCl2, 10 μM ATP, 500 nM substrate peptide (biotin-aminohexylAEEEEYMMMMAKKKK-NH2; QPC), and 0.5 nM activated enzyme. Reactions are stopped after 1 hour at room temperature with 33 μM EDTA. Peptide phosphorylation is measured by time-resolved fluorescence resonance energy transfer with 7 nM streptavidin Surelight allophycocyanin and 1 nM europium-conjugated phosphotyrosine antibodies. Plates are read in a multilabel reader.
细胞实验 Cells are seeded in 96-well plates and incubated overnight at 37 °C, and treated with various concentrations of GSK1904529A for 72 hours. For the NIH-3T3/LISN, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 hours. The tissue culture medium is replaced with serum-free medium and the cells are treated with DMSO or GSK1904529A for 2 hours. IGF-I (30 ng/mL) is added and the cells are incubated at 37 °C for 72 hours. Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are determined.</(Only for Reference)
别名 GSK 4529
分子量 851.96
分子式 C44H47F2N9O5S
CAS No. 1089283-49-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 114 mg/mL (133.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1738 mL 5.8688 mL 11.7376 mL 29.3441 mL
5 mM 0.2348 mL 1.1738 mL 2.3475 mL 5.8688 mL
10 mM 0.1174 mL 0.5869 mL 1.1738 mL 2.9344 mL
20 mM 0.0587 mL 0.2934 mL 0.5869 mL 1.4672 mL
50 mM 0.0235 mL 0.1174 mL 0.2348 mL 0.5869 mL
100 mM 0.0117 mL 0.0587 mL 0.1174 mL 0.2934 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Sabbatini P, et al. Clin Cancer Res, 2009, 15(9), 3058-3067.

文献引用

1. Guan J, Borenäs M, Xiong J, et al.IGF1R Contributes to Cell Proliferation in ALK-Mutated Neuroblastoma with Preference for Activating the PI3K-AKT Signaling Pathway.Cancers.2023, 15(17): 4252.
B-Raf IN 15 Raf inhibitor 3 Cyclorasin 9A5 SOS1-IN-11 B-Raf IN 16 Dabrafenib RAF709 B-Raf IN 11

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌活性化合物库 含氟化合物库 抗衰老化合物库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

GSK1904529A 1089283-49-7 Angiogenesis Apoptosis MAPK Tyrosine Kinase/Adaptors VEGFR Raf Syk IGF-1R Insulin Receptor Inhibitor anti-tumor GSK4529 GSK-1904529A inhibit insulin GSK 4529 GSK-4529 inhibitor

 

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