CAS NO: | 443798-47-8 |
包装 | 价格(元) |
10mM 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 443798-47-8 |
化学名 | 5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide |
Canonical SMILES | NC1=NC(NC2=CC=C(S(N)(=O)=O)C=C2)=NN1C(NC3=C(F)C=CC=C3F)=S |
分子式 | C15H13F2N7O2S2 |
分子量 | 425.4 |
溶解度 | ≤10mg/ml in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 0.6 and 0.5 nM forCdk1/cyclin B and Cdk2/cyclin A, respectively Cdk1/2 Inhibitor III is a Cdk inhibitor. Cyclin-dependent kinases (CDKs) are a family members of serine-threonine protein kinases responsible for regulation of the eukaryotic cell cycle. Their timed activation guides cells via the cell cycle and ensures the accurate execution of cell division. In vitro: Cdk1/2 Inhibitor III was identified as a cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A and could less potently inhibit CDC2-like kinases 1 and 3, VEGFR2, and GSK-3β. Cdk1/2 Inhibitor III was found to be lack of effect against a panel of other kinases. Moreover, Cdk1/2 Inhibitor III could block the growth of various cancer cell lines (IC50 values range from 20 to 92 nM) [1]. In vivo: The in-vivo efficacy of compound 3b, a structurally close Cdk1/2 Inhibitor III analog, was examined in the A375 human melanoma cell xenograft model. Doses at 125, 100, and 75 mg/kg were administered once a day for 32 days and tumor size was measured every 4 days. The results showed that in the 125 mg/kg group, there was one nontreatment-related death but the remaining four animals experienced stable disease. In addition, compound 3b administered at 100 and 75 mg/kg led to mean day of survival values of 50.1 and 48.5 days, respectively, with only one treatment-related death in the 100 mg/kg group [1]. Clinical trial: So far, no clinical study has been conducted. Reference: |