5.33063

VPS34 Inhibitor, SAR405

• Sinônimo(s): VPS34 Inhibitor, SAR405, Vacuolar Protein Sorting 34 Inhibitor, SAR405, (S)-1-((5-chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one
• Fórmula empírica (Notação de Hill): C₁₉H₂₁ClF₃N₅O
• Número CAS: 1523406-39-4
• Peso molecular: 427.85
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥96% (HPLC)
• Nível de qualidade: 100
• forma: powder
• potência: 1.5 nM K_i
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: off-white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

A cell-permeable pyrimido[1,2-a]pyrimidin-6(2H)-one derivative that acts as a potent, selective, and ATP competitive inhibitor of vacuolar protein sorting 34 kinase activity (Vps34; K_d = 1.5 nM, IC₅₀ = 1.2 nM in a biochemical assay, and IC₅₀ = 27 nM in a cell based assay). Does not affect the activity of over 200 other protein kinases including class I and II PI 3 kinases and mTOR (~ 10 µM). However, it displays a weak inhibitory activity against SMG1 at higher concentrations (IC₅₀ = 1 µM). Does not affect the Akt phosphorylation even at higher concentrations (~10 µM), Shown to affect the late endosome-lysosome compartment formation and block the formation of autophagosomes in starved HeLa and H1299 cells (~ 1 µM). Acts synergistically with everolimus to block the proliferation of ACHN and 786-O renal tumor cells.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
VPS34

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Ronan, B., et al. 2014. Nat. Chem. Biol.10, 1013.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable