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。
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 | A11313 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 418.7 |
| Formula | C16H17Cl2N5O2.HCl |
| 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. | 902135-91-5 |
| Synonyms | AT 7519, AT-7519 |
| SMILES | C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl.Cl |
溶解度
| In vitro (25°C) | DMSO | Warmed: 49 mg/mL (117.03 mM) |
| Water | Warmed: 40 mg/mL (95.53 mM) |
| Ethanol | Warmed: 26 mg/mL (62.09 mM) |
| In vivo | Saline | 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 23.88 mL | 119.42 mL | 238.83 mL |
| 0.5 mM | 4.78 mL | 23.88 mL | 47.77 mL |
| 1 mM | 2.39 mL | 11.94 mL | 23.88 mL |
| 5 mM | 0.48 mL | 2.39 mL | 4.78 mL |
*The above data is based on the productmolecular weight 418.7 . 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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