ChemicalBook CAS数据库列表 GSK1838705A
GSK1838705A
- CAS号:1116235-97-2
- 英文名:GSK1838705A
- 中文名:GSK1838705A
- CBNumber:CB72605356
- 分子式:C27H29FN8O3
- 分子量:532.57
- MOL File:1116235-97-2.mol
GSK1838705A化学性质
- 密度 :1.399
- 储存条件 :-20°C
- 溶解度 :DMSO: soluble20mg/mL, clear
- 形态 :powder
- 酸度系数(pKa) :13.27±0.50(Predicted)
- 颜色 :white to light brown
安全信息
- WGK Germany :3
GSK1838705A性质、用途与生产工艺
- 生物活性 GSK1838705A是一种有效的IGF-1R抑制剂，IC50为2.0 nM，适度有效作用于IR和ALK，IC50分别为1.6 nM和0.5 nM，对其他蛋白激酶几乎没有作用活性。
- 体外研究 GSK1838705A potently and ATP-competitively inhibits IGF-1R and IR with appKi values of 0.7 nM and 1.1 nM, respectively.In cells, GSK1838705A potently inhibits ligand-induced phosphorylation of IGF-1R and IR with IC50 of 85 nM and 79 nM, respectively. GSK1838705A shows the significant anti-proliferative effect in a panel of cell lines derived from solid and hematologic tumors such as L-82, SUP-M2, SK-ES and MCF-7 cells with EC50 of 24 nM, 28 nM, 141 nM and 203 nM, respectively. GSK1838705A shows an accumulation of MCF-7 and NCl-H929 cells predominantly in G1 (2N) phase of the cell cycle. GSK1838705A also inhibits ALK with Ki of 0.35 nM and supresses the proliferation of nucleophosmin (NPM)-ALK fusion cells with EC50 of 24-88 nM. GSK1838705A potently inhibits NPM-ALK phosphorylation in Karpas-299 and SR-786 cells, while has modest effect on STAT3 phosphorylation.
- 体内研究 In NIH-3T3/LISN tumor-bearing mice, oral treatment of GSK1838705A (60 mg/kg) cause tumor growth inhibition by 77%, without significant weight loss. In COLO 205 tumor-bearing mice, inhibition of tumor growth by GSK1838705A (30 mg/kg) is 80%. Besides, the antitumor efficacy of GSK1838705A is also observed in mice bearing HT29 xenograft or BxPC3 xenograft. In mice, GSK1838705A (60 mg/kg) leads to a transient 2-fold increase in blood glucose levels by inhibiting IR signaling. GSK1838705A (60 mg/kg) inhibits the growth of established Karpas-299 xenografts with 93% tumor growth inhibition, with no effect on weights of the rats.
- 特征 GSK1838705A is a small-molecule kinase inhibitor of IGF-1R and the insulin receptor.
- 生物活性 GSK1838705A是一种有效的IGF-1R抑制剂，IC50为2.0 nM，适度有效作用于IR和ALK，IC50分别为1.6 nM和0.5 nM，对其他蛋白激酶几乎没有作用活性。
-
靶点
Target Value ALK
(Cell-free assay)0.5 nM Insulin Receptor
(Cell-free assay)1.6 nM IGF-1R
(Cell-free assay)2 nM -
体外研究
GSK1838705A有效且ATP竞争性抑制IGF-1R和IR，
- 体内研究 在负荷NIH-3T3/LISN肿瘤的小鼠体内，GSK1838705A (60 mg/kg)口服治疗抑制77%肿瘤生长，而没有显著的体重损失。在负荷COLO 205肿瘤的小鼠体内，GSK1838705A (30 mg/kg)能够抑制80%的肿瘤生长。此外，GSK1838705A的抗肿瘤作用在负荷HT29异种移植物或BxPC3异种移植物的小鼠体内也能观察到。在小鼠体内，GSK1838705A (60 mg/kg)通过抑制IR信号，引起血糖水平短暂增加2倍。GSK1838705A (60 mg/kg)抑制已建立的Karpas-299异种移植物的生长，抑制率为93%，而对大鼠的体重没有影响。
GSK1838705A上下游产品信息
上游原料
下游产品
GSK1838705A 试剂级价格
- 更新日期：2024/11/08
- 产品编号：HY-13020
- 产品名称：GSK1838705A
- CAS编号：
- 包装：1 mg
- 价格：351元
- 更新日期：2024/11/08
- 产品编号：HY-13020
- 产品名称：GSK1838705A GSK1838705A
- CAS编号：1116235-97-2
- 包装：5mg
- 价格：900元
GSK1838705A生产厂家
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
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