| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G407919-1ml |
1ml |
现货  |
|
| 英文别名 | 3-(4-(4-(2-(3-((dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | GSK1070916 |
| 生化机理 | GSK1070916 是一种 Aurora B/C 的可逆 ATP 竞争性抑制剂，IC50 为 3.5 nM/6.5 nM。它对密切相关的 Aurora A-TPX2 复合物的选择性大于 100 倍。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 | 丝氨酸/苏氨酸蛋白激酶 Aurora-C 抑制剂 |
| 产品介绍 |
GSK1070916是可逆的ATP竞争性Aurora B和C抑制剂，IC50分别为3.5 nM和6.5 nM。而对于Aurora A-TPX2复合物的IC50则为490 nM。 Information GSK1070916 is a reversible and ATP-competitive inhibitor ofAurora B/CwithIC50of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1. GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis. In another study, it is also reported high chromosome number associated with resistance to the inhibition of Aurora B and C suggests cells with a mechanism to bypass the high ploidy checkpoint are resistant to GSK1070916. In vivo GSK1070916 (25, 50, or 100 mg/kg) shows dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. cell lines： Concentrations：0-15 mM Incubation Time：6-7 days Powder Purity:≥97% |
| IC50 | Aurora B-INCENP, IC50: 3.5 nM |
|---|---|
| ALogP | 4.841 |
| hba_count | 3 |
| HBD Count | 2 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC[N]1C=C(C2=C3C=C([NH]C3=NC=C2)C4=CC=CC(=C4)CN(C)C)C(=N1)C5=CC=C(NC(=O)N(C)C)C=C5 |
| 分子量 | 507.63 |
| Reaxy-Rn | 15498355 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15498355&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 85 mg/mL (197.86 mM); Ethanol: 85 mg/mL (197.86 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 93 |
| DMSO(mM) Max Solubility | 183.2 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 15498355 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15498355&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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