| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C408469-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(2-amino-4-methylthiazol-5-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | CYC116 |
| 生化机理 | CYC116 是 Aurora A/B 的强效抑制剂，Ki为 8.0 nM/9.2 nM，对 VEGFR2 的作用较弱（Ki为 44 nM），比 CDK 的作用强 50 倍，对 PKA、Akt/PKB、PKC 无活性，对 GSK-3α/β、CK2、Plk1 和 SAPK2A 无影响。第 1 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 | 血管内皮生长因子受体 2 抑制剂 |
| 产品介绍 |
Information CYC116 is a potent inhibitor ofAurora A/BwithKiof 8.0 nM/9.2 nM, is less potent to VEGFR2 (Kiof 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1. The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. In vivo Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. cell lines：K562 cell lines Concentrations：0-10 μM Incubation Time：72 or 96 hours Powder Purity:≥98% |
| ALogP | 2.6 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4 |
| 分子量 | 368.46 |
| Reaxy-Rn | 11324028 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11324028&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 69 mg/mL (219.95 mM); Ethanol: 25 mg/mL (79.69 mM); Water: ˂1 mg/mL |
|---|
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