| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| V408523-1ml |
1ml |
现货  |
|
| 英文别名 | 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Vistusertib (AZD2014) |
| 生化机理 | Vistusertib（AZD2014）是一种新型 mTOR 抑制剂，在无细胞试验中的 IC50 值为 2.8 nM；对多种 PI3K 同工酶（α/β/γ/δ）具有高度选择性。当测试浓度为 1 μM 时，AZD2014 与大多数激酶没有结合或结合较弱。AZD2014 可诱导 HCC 细胞增殖抑制、凋亡、细胞周期停滞和自噬，并具有抗肿瘤活性。 |
| 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 | 丝氨酸/苏氨酸蛋白激酶 mTOR 抑制剂 |
| 产品介绍 |
AZD2014是高效mTOR抑制剂，IC50为2.8 nM，对PI3K各亚型(α/β/γ/δ)的抑制性较弱。A selective inhibitor of mTOR kinase Information Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. In vivo AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates. cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CNC(=O)C1=CC=CC(=C1)C2=CC=C3C(=N2)N=C(N=C3N4CCOCC4C)N5CCOCC5C |
| 分子量 | 462.54 |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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