GSK1904529A

产品详情：

发布时间： 2024-07-15 12:30:04

CAS号：1089283-49-7

常用名： N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc. IC50 value: 27/25 nM (IGF1R/IR) [1]Target: IGF1R/IRin vitro: 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].in vivo: 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]. 物理化学性质： CAS号：1089283-49-7 常用中文名：N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺常用英文名：GSK1904529A 分子式：C44H47F2N9O5S 分子量：851.963 密度：1.4±0.1 g/cm3 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：-20℃

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公司名：上海念兴实业有限公司推荐

认证状态： 已认证供应商

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2022-03-04 价格：￥1287.9 GSK1904529A

2018-04-16 价格：￥需询单 GSK1904529A

2020-12-08 价格：￥1425.0 GSK1904529A

2023-08-31 价格：￥需询单 GSK1904529A

2024-05-20 价格：￥需询单 GSK1904529A

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N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺价格

GSK1904529A

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