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Cdk1/2 Inhibitor III

Product Name
Cdk1/2 Inhibitor III
CAS No.
443798-47-8
Chemical Name
Cdk1/2 Inhibitor III
Synonyms
K00546;K00546 (K 00546);5-Amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide;1H-1,2,4-Triazole-1-carbothioamide, 5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-
CBNumber
CB64666985
Molecular Formula
C15H13F2N7O2S2
Formula Weight
425.44
MOL File
443798-47-8.mol
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Cdk1/2 Inhibitor III Property

Boiling point:
649.1±65.0 °C(Predicted)
Density 
1.72±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤10mg/ml in DMSO
form 
solid
pka
6.61±0.70(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18859
Product name
Cdk1/2 Inhibitor III
Packaging
1mg
Price
$97
Updated
2024/03/01
Cayman Chemical
Product number
18859
Product name
Cdk1/2 Inhibitor III
Packaging
10mg
Price
$578
Updated
2024/03/01
Cayman Chemical
Product number
18859
Product name
Cdk1/2 Inhibitor III
Packaging
5mg
Price
$384
Updated
2024/03/01
TRC
Product number
C228138
Product name
Cdk1/2InhibitorIII
Packaging
2.5mg
Price
$185
Updated
2021/12/16
ChemScene
Product number
CS-0028811
Product name
K00546
Purity
98.78%
Packaging
5mg
Price
$280
Updated
2021/12/16
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Cdk1/2 Inhibitor III Chemical Properties,Usage,Production

Description

Cyclin-dependent kinases (Cdks) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Cdk1/2 Inhibitor III is a cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50s = 0.6 and 0.5 nM, respectively). It less potently inhibits CDC2-like kinases 1 and 3, VEGFR2, and GSK-3β (IC50s = 8.9, 29, 32, and 140 nM, respectively) and is without effect against a panel of other kinases. Cdk1/2 Inhibitor III blocks the growth of several cancer cell lines (IC50 values range from 20 to 92 nM).

Uses

Cdk1/2 Inhibitor III is a cyclin-?dependent kinase (CDK) inhibitor. Cdk1 and Cdk2 performs inhibitory activities, and in vitro cellular proliferation in various human tumor cells.

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].

IC 50

0.6 and 0.5 nm forcdk1/cyclin b and cdk2/cyclin a, respectively

References

[1] lin, r. ,connolly, p.j.,huang, s., et al. 1-acyl-1h-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. journal of medicinal chemistry 48(13), 4208-4211 (2005).

Cdk1/2 Inhibitor III Preparation Products And Raw materials

Raw materials

Preparation Products

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Cdk1/2 Inhibitor III Suppliers

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443798-47-8, Cdk1/2 Inhibitor IIIRelated Search:


  • K00546 (K 00546)
  • K00546
  • 1H-1,2,4-Triazole-1-carbothioamide, 5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-
  • 5-Amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
  • 443798-47-8