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别名 OTS167, MELK inhibitor
OTSSP167 (OTS167) 是一种高效的,ATP 竞争性的 MELK 抑制剂,其 IC50=0.41 nM。

OTSSP167 (OTS167) 是一种高效的,ATP 竞争性的 MELK 抑制剂,其 IC50=0.41 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 328 | In stock | |
| 2 mg | ¥ 478 | In stock | |
| 5 mg | ¥ 828 | In stock | |
| 10 mg | ¥ 1,230 | In stock | |
| 25 mg | ¥ 1,930 | In stock | |
| 50 mg | ¥ 2,970 | In stock | |
| 100 mg | ¥ 4,460 | In stock | |
| 500 mg | ¥ 9,290 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 897 | In stock |
OTSSP167 相关产品
| 产品描述 | OTSSP167 (OTS167) is an orally available inhibitor of maternal embryonic leucine zipper kinase (MELK) with potential antineoplastic activity. |
| 靶点活性 | MELK:0.41 nM |
| 体外活性 | 在MDA-MB-231模型中,每天一次口服10 mg/kg OTSSP167显示对TGI 72%的生长抑制率.OTSSP167以静脉内和口服两种方式处理小鼠,异种移植研究中显示出对乳房、肺、前列腺和胰腺癌细胞系的显著肿瘤生长抑制作用.OTSSP167作用于多种癌症类型,具有剂量依赖性及MELK依赖性,对体重减轻没有或很少有影响. |
| 体内活性 | OTSSP167抑制PSMA1和DBNL的磷酸化,PSMA1和DBNL是新型MELK底物,对干细胞的特征和侵袭性是至关重要的。OTSSP167通过抑制PSMA1磷酸化抑制乳腺癌细胞的球形成。OTSSP167抑制MELK高水平表达的A549、T47D、DU4475和22Rv1 癌细胞,IC50分别为6.7,4.3,2.3和6.0 nM。 |
| 激酶实验 | in vitro kinase assay: MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl2, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-32P]ATP for 30 min at 30 °C. The reaction is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation. |
| 细胞实验 | Cell Counting Kit-8(Only for Reference) |
| 别名 | OTS167, MELK inhibitor |
| 分子量 | 487.42 |
| 分子式 | C25H28Cl2N4O2 |
| CAS No. | 1431697-89-0 |
| Smiles | CN(C)C[C@H]1CC[C@@H](CC1)Nc1c(cnc2ccc(nc12)-c1cc(Cl)c(O)c(Cl)c1)C(C)=O |
| 密度 | no data available |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | DMSO: 7.22 mg/mL (14.81 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
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DMSO
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