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化學性質:
規格 | 10mM 1 mL in DMSO 5mg 10mg 50mg 100mg |
CAS | 443798-47-8 |
別名 | N/A |
化學名 | 5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide |
分子式 | C15H13F2N7O2S2 |
分子量 | 425.4 |
溶解度 | ≤10mg/ml in DMSO |
儲存條件 | Store at -20°C |
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 |
產品描述:
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.
特別提醒:
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區。
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278