| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T407937-1ml |
1ml |
现货  |
|
| 英文别名 | 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | TAK-901 |
| 生化机理 | TAK-901 是一种新型 Aurora A/B 抑制剂，IC50 为 21 nM/15 nM。它不是细胞 JAK2、c-Src 或 Abl 的强效抑制剂。第一阶段 |
| 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 Aurora-B 抑制剂 |
| 产品介绍 |
TAK-901是多靶点的的极光激酶 (aurora)抑制剂，对极光激酶A和B的IC50 值分别为21 和15 nM。 Information TAK-901 is a novel inhibitor ofAurora A/BwithIC50of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1. TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901 binding to Aurora B-INCENP is determined to be 0.02 nM. TAK-901 induces inhibition of cell proliferation in cultured human cancer cell lines from different tissues with IC50s ranging from 40 to 500nM. Consistent with Aurora B inhibition, TAK-901 treatment produces polyploidy in human PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured by immunofluorescence and flow cytometry. Examination of a broad panel of kinases reveals that multiple kinases, including FLT3, FGFR and the Src family kinases, are inhibited by TAK-901 with IC50 values similar to those for Aurora A and B. In cells, TAK-901 suppresses the Flt3 and FGFR2 autophosphorylation with IC50 values close to that of Aurora B as measured by cellular histone H3 phosphorylation, whereas the IC50s for inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of pathway specific reporter-based cell models, TAK-901 inhibits the NFkB and JAK/STAT pathways with submicromolar potency. In vivo
cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| ALogP | 4.5 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CCS(=O)(=O)C1=CC=CC(=C1)C2=CC(=C(C3=C2C4=C(N3)N=CC(=C4)C)C)C(=O)NC5CCN(CC5)C |
| PubChem CID | 16124208 |
| 分子量 | 504.66 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 63 mg/mL (200.72 mM); Ethanol: 24 mg/mL (76.46 mM); Water: Insoluble; |
|---|
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