| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G408364-1ml |
1ml |
现货  |
|
| 英文别名 | 2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | GSK1838705A |
| 生化机理 | GSK1838705A 是一种强效的 IGF-1R 抑制剂，IC50 为 2.0 nM，对 IR 和 ALK 的抑制作用不大，IC50 分别为 1.6 nM 和 0.5 nM，对其他蛋白激酶的活性很小。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | ALK 受体酪氨酸激酶抑制剂；胰岛素样生长因子 I 受体抑制剂；胰岛素受体抑制剂；核糖体蛋白 S6 激酶 A1 抑制剂 |
| 产品介绍 |
GSK1838705A是IGF-IR，InsR和ALK抑制剂，IC50分别为2.0，1.6和0.5 nM。 Information GSK1838705A GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases. 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. In vivo 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. cell lines：HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, HepG2, MCF-7, MDA-MB-468 and BT-474 cell lines Concentrations：0 to 10 μM Incubation Time：72 hours Powder Purity:≥96% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)OC |
| 关联CAS | 1116235-97-2 |
| MeSH Entry Terms | GSK 1838705A;GSK-1838705A;GSK1838705A |
| 分子量 | 532.57 |
| Reaxy-Rn | 18983141 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18983141&ln= |
| WGK Germany | 3 |
|---|
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