Cdk1/2 Inhibitor III

Cdk1/2 Inhibitor III

Catalog Number:
L002372874APE
Mfr. No.:
APE-C3679
Price:
$286
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      • Overview
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          Background

          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.

      • Properties
        • Alternative Name
          5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
          CAS Number
          443798-47-8
          Molecular Formula
          C15H13F2N7O2S2
          Molecular Weight
          425.4
          Appearance
          A solid
          Purity
          Purity ≥95.00%
          Solubility
          ≤10mg/ml in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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