528117

PI 3-K inhibitor IX, PIK-90

The PI 3-K inhibitor IX, PIK-90, also referenced under CAS 677338-12-4, controls the biological activity of PI 3-K. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): PI 3-K inhibitor IX, PIK-90, N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
• Fórmula empírica (Notação de Hill): C₁₈H₁₇N₅O₃
• Número CAS: 677338-12-4
• Peso molecular: 351.36
• Número MDL: MFCD12910483
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: pale yellow
• solubilidade: DMSO: 0.5 mg/mL
• Condições de expedição: wet ice
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: [n]21[c](c3c(nc2NC(=O)c4cnccc4)c(c(cc3)OC)OC)=NCC1
• InChI: 1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)
• chave InChI: ZJAVHOMVDCMAMF-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC₅₀ = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC₅₀ = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC₅₀ = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC₅₀ = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC₅₀ >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Nota de preparo

Slight warming may be required to for complete solubility.

Reconstituição

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

Outras notas

Fan, Q.W., et al. 2007. Cancer Res.67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell9, 341.
Knight, Z.A., et al. 2006. Cell125, 733.

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