
簡要描述:INK-128 1224844-38-5INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.
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| 品牌 | absin | CAS | 1224844-38-5 |
|---|---|---|---|
| 分子式 | C15H15N7O | 純度 | >98% |
| 分子量 | 309.33 | 貨號 | abs810344 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent and selective mTOR inhibitor | 應用領域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
INK-128 1224844-38-5
| 產(chǎn)品描述 | |
| 描述 | INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms. |
| 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 | 沙帕色替;INK 128; INK128;Sapanisertib; MLN0128 |
| 外觀 | 白色至類白色固體 |
| 可溶性/溶解性 | DMSO : 58 mg/mL (187.5 mM) Ethanol : 2 mg/mL (6.46 mM) |
| 生物活性 | |
| 靶點 | mTOR;mTORC1;mTORC2;PI3Kα;PI3Kγ;PI3Kδ |
| In vitro(體外研究) | INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. |
| In vivo(體內(nèi)研究) | In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. |
| 研究領域 | |
| 研究領域 | CancerCell cycleCell cycle inhibitorsOther CardiovascularHeartCardiogenesisTranscription factors/regulators Cell CycleCell Cycle InhibitorsOther EpigeneticsDNA / RNADNA Damage & RepairDNA Damage ResponseDNA Damage Recognition MetabolismTypes of diseaseObesity NeuroscienceDevelopment NeuroscienceProcesses Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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