
簡要描述:GSK-2636771 1372540-25-4GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
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| 品牌 | absin | CAS | 1372540-25-4 |
|---|---|---|---|
| 分子式 | C22H22F3N3O3 | 純度 | >98% |
| 分子量 | 433.42 | 貨號 | abs810341 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent, orally bioavailable | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
GSK-2636771 1372540-25-4
| 產(chǎn)品描述 | |
| 描述 | GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a. |
| 純度 | >98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | GSK 2636771,GSK-2636771 |
| 外觀 | Powder |
| 可溶性/溶解性 | DMSO 28 mg/mL (64.6 mM) |
| 生物活性 | |
| 靶點 | PI3Kβ |
| In vitro(體外研究) | GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. |
| In vivo(體內(nèi)研究) | GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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