生物活性
AT7519是多种细胞周期蛋白依赖性激酶（CDK）的抑制剂，可导致细胞周期停滞，诱导细胞凋亡和抑制肿瘤细胞增殖。作用于CDK1，2，4，6和9时，IC50为10-210 nM，对CDK3作用效果稍弱，对CDK7几乎没有抑制活性。
Targets
| Target | Value |
| CDK9/CyclinT | IC50:<10nM |
| CDK5/p35 | IC50: 13nM |
| CDK2/CyclinA | IC50: 47nM |
| GSK-3β | IC50: 89nM |
| CDK4/CyclinD1 | IC50: 100nM |
| CDK6/CyclinD3 | IC50: 170nM |
| CDK1/CyclinB | IC50: 210nM |
| CDK3/CyclinE | IC50: 360nM |
| PI3Kβ | IC50: >1μM |
| PLK3 | IC50: >1μM |
| RET | IC50: >1μM |
| SGK | IC50: >1μM |
| TrkB | IC50: >1μM |
| JAK2 | IC50: >1μM |
| CDK7/CyclinH/MAT1 | IC50: 2.4μM |
| SAPK2A(p38α) | IC50: >10μM |
| p70S6K | IC50: >10μM |
| PDGFR | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PKBβ | IC50: >10μM |
| VEGFR1 | IC50: >10μM |
| AuroraA | IC50: >10μM |
| c-Abl | IC50: >10μM |
| c-Src | IC50: >10μM |
| Chk1 | IC50: >10μM |
| EGFR | IC50: >10μM |
| FGFR3 | IC50: >10μM |
| IR | IC50: >10μM |
| JNK2 | IC50: >10μM |
| MAPK1 | IC50: >10μM |
| MEK1 | IC50: >10μM |
| Met | IC50: >10μM |
化学数据
| 目录号 | A10093 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 382.2 |
| Formula | C16H17Cl2N5O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 844442-38-2 |
| Synonyms | AT-7519 |
| SMILES | C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl |
溶解度
| In vitro (25°C) | DMSO | 9 mg/mL (23.54 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+30% PEG 300+2% Tween 80+ddH2O | 1 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 26.16 mL | 130.82 mL | 261.64 mL |
| 0.5 mM | 5.23 mL | 26.16 mL | 52.33 mL |
| 1 mM | 2.62 mL | 13.08 mL | 26.16 mL |
| 5 mM | 0.52 mL | 2.62 mL | 5.23 mL |
*The above data is based on the productmolecular weight 382.2. 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.
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