5.31976

MPS1 Inhibitor III, AZ3146

• Sinonimo/i: MPS1 Inhibitor III, AZ3146, AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
• Formula empirica (notazione di Hill): C₂₄H₃₂N₆O₃
• Numero CAS: 1124329-14-1
• Peso molecolare: 452.55
• Numero MDL: MFCD18384959
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Potenza: ~35 nM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: purple
• Solubilità: DMSO: 5 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: 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); YUKWVHPTFRQHMF-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable