5.31976

MPS1 Inhibitor III, AZ3146

• Synonyme(s) : MPS1 Inhibitor III, AZ3146, AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
• Formule empirique (notation de Hill): C₂₄H₃₂N₆O₃
• Numéro CAS: 1124329-14-1
• Poids moléculaire : 452.55
• Numéro MDL: MFCD18384959
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: ~35 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: purple
• Solubilité: DMSO: 5 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: N1(CCC(CC1)Oc2cc(c(cc2)Nc3nc4[n]([c]([n](c4cn3)C)=O)C5CCCC5)OC)C
• InChI: 1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27)
• Clé InChI: YUKWVHPTFRQHMF-UHFFFAOYSA-N

Description

Description générale

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1; IC₅₀ = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1; IC₅₀ = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Hewitt, L., et al. 2010. Jour. Cell Biol.190, 25.

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 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable