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443798-55-8

443798-55-8 Structure

443798-55-8 Structure
IdentificationBack Directory
[Name]

CDK1/2InhibitorIII
[CAS]

443798-55-8
[Synonyms]

2 Inhibitor III
CDK1/2InhibitorIII
Cdk-1/2 Inhibitor III,Cdk1/2 Inhibitor III
5-amino-N-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide
1H-1,2,4-Triazole-1-carbothioamide, 3-amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-
[Molecular Formula]

C15H13F2N7O2S2
[MOL File]

443798-55-8.mol
[Molecular Weight]

425.44
Chemical PropertiesBack Directory
[Boiling point ]

649.1±65.0 °C(Predicted)
[density ]

1.72±0.1 g/cm3(Predicted)
[storage temp. ]

+2C to +8C
[solubility ]

DMSO: 10mg/mL
THF: soluble
acetone: soluble
[form ]

White solid
[pka]

6.61±0.70(Predicted)
[color ]

white
Hazard InformationBack Directory
[Uses]

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]

Cyclin-dependent kinases (CDKs) are protein kinases and involved with the regulation of the cell cycle. CDK 1/2 inhibitor III selectively inhibits CDK1 and CDK2. Studies have shown that CDK 1/2 Inhibitor III can also inhibit in vitro cellular proliferation in various human tumor cells.
[General Description]

A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50 = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC50 = 32 nM), GSK-3β (IC50 = 140 nM), and a panel of eight other kinases (IC50 ≥ 1 μM).
[Biochem/physiol Actions]

Cell permeable: yes
[IC 50]

Cdk1/cyclin B: 2.1 μM (IC50)
Spectrum DetailBack Directory
[Spectrum Detail]

CDK1/2InhibitorIII(443798-55-8)1HNMR
443798-55-8 suppliers list
Company Name: Shanghai EFE Biological Technology Co., Ltd.  
Telephone: 021-65675885 18964387627
Website: http://www.efebio.com
Company Name: Energy Chemical  
Telephone: 021-58432009 400-005-6266
Website: http://www.energy-chemical.com
Company Name: cjbscvictory  
Telephone: 13348960310 13348960310
Website: www.weikeqi-biotech.com/
Company Name: TargetMol Chemicals Inc.  
Telephone: 4008200310 15002144251
Website: https://www.targetmol.cn/
Company Name: Shandong Dayou Pharmaceutical Research and Development Co., Ltd.  
Telephone: dayouchem@126.com 15165037910
Website:
Company Name: Shanghai Amole Biotechnology Co., Ltd.  
Telephone: 13370042665 18916960931
Website: www.amole.com.cn/
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