217714

Cdk1/2 Inhibitor III

The Cdk1/2 Inhibitor III, also referenced under CAS 443798-55-8, controls the biological activity of Cdk1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Cdk1/2 Inhibitor III, 5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
• Formule empirique (notation de Hill) : C₁₅H₁₃F₂N₇O₂S₂
• CAS Number: 443798-55-8
• Poids moléculaire : 425.44
• Numéro MDL: MFCD09264159
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 10 mg/mL; THF: soluble; acetone: soluble
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: Fc1c(c(ccc1)F)NC(=S)[n]2nc(nc2N)Nc3ccc(cc3)[S](=O)(=O)N
• InChI: 1S/C15H13F2N7O2S2/c16-10-2-1-3-11(17)12(10)21-15(27)24-13(18)22-14(23-24)20-8-4-6-9(7-5-8)28(19,25)26/h1-7H,(H,21,27)(H2,19,25,26)(H3,18,20,22,23)
• Clé InChI: ARIOBGGRZJITQX-UHFFFAOYSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Cdk1/cyclin B, Cdk2/cyclin A

Product competes with ATP.

Reversible: yes

Target IC₅₀: 20 nM, 35 nM and 92 nM for anti-proliferative properties in HCT-116, HeLa, and A375 cells, respectively; 600 pM and 500 pM, against Cdk1/cyclin B and Cdk2/cyclin A, respectively

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Lin, R., et al. 2005.J. Med. Chem.48, 4208.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable