528116

PI 3-Kα Inhibitor VIII

The PI 3-Kα Inhibitor VIII controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: PI 3-Kα Inhibitor VIII, N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-Nʹ-methyl-Nʹʹ-(2-methyl-5-nitrobenzene)sulfonohydrazide, HCl, PIK-75, PI 3-K Inhibitor VIII
• Fórmula empírica (notación de Hill): C₁₆H₁₄BrN₅O₄S · 2H₂O · xHCl
• Número de CAS: 372196-77-5
• Peso molecular: 488.31 (free base basis)
• Número MDL: MFCD12546130
• Código UNSPSC: 12352200
• NACRES: NA.28

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: pale yellow
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: [S](=O)(=O)(N(\N=C\c2[n]3c(nc2)ccc(c3)Br)C)c1c(ccc(c1)[N+](=O)[O-])C.Cl
• InChI: 1S/C16H14BrN5O4S.ClH/c1-11-3-5-13(22(23)24)7-15(11)27(25,26)20(2)19-9-14-8-18-16-6-4-12(17)10-21(14)16;/h3-10H,1-2H3;1H/b19-9+;
• Clave InChI: VOUDEIAYNKZQKM-MYHMWQFYSA-N

Descripción

Descripción general

A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI3-K inhibitor (IC₅₀ = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC₅₀ ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).

Envase

Packaged under inert gas

Advertencia

Toxicity: Regulatory Review (Z)

Reconstitución

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

Otras notas

Kim, S., et al. 2007. Blood110, 4206.
Hayakawa, M., et al. 2007. Bioorg. Med. Chem.15, 5837.
Knight, Z.A., et al. 2007. Cell125, 733.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable