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GSK1070916是一种有效的Aurora B/C激酶抑制剂（IC50为3.5 nM/6.5 nM），在组织培养细胞和人肿瘤异种移植模型中具有广泛的抗肿瘤活性。
Targets
| Target | Value |
|---|---|
| AuroraB-INCENP | IC50: 3.5nM |
| AuroraC-INCENP | IC50: 6.5nM |
| FLT1 | IC50: 42nM |
| Tie-2 | IC50: 59nM |
| SIK | IC50: 70nM |
| FLT4 | IC50: 74nM |
| FGFR1 | IC50: 76nM |
| AuroraA-TPX2 | IC50: 1.1μM |
| In vitro (25°C) | DMSO | 91 mg/mL (179.26 mM) | |
| Water | Insoluble | ||
| Ethanol | 8 mg/mL (15.75 mM) | ||
| In vivo | 2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0 | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 19.7 mL | 98.5 mL | 196.99 mL |
| 0.5 mM | 3.94 mL | 19.7 mL | 39.4 mL |
| 1 mM | 1.97 mL | 9.85 mL | 19.7 mL |
| 5 mM | 0.39 mL | 1.97 mL | 3.94 mL |
*The above data is based on the productmolecular weight 507.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 目录号 | A11168 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 507.63 |
| Formula | C30H33N7O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 942918-07-2 |
| Synonyms | GSK-1070916 |
| SMILES | CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC(=CC=C5)CN(C)C |
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