528121

PI 3-K/PDK-1 Inhibitor, NVP-BAG956

The PI 3-K/PDK-1 Inhibitor, NVP-BAG956, also referenced under CAS 853910-02-8, controls the biological activity of PI 3-K/PDK-1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: PI 3-K/PDK-1 Inhibitor, NVP-BAG956, α,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile, BAG956, PI 3-K Inhibitor XVI, PDK1 Inhibitor IV
• Fórmula empírica (notación de Hill): C₂₈H₂₁N₅
• Número de CAS: 853910-02-8
• Peso molecular: 427.50
• Código UNSPSC: 12352200

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: orange
• solubilidad: DMSO: 25 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C28H21N5/c1-19-32-26-17-31-25-13-8-20(6-7-21-5-4-14-30-16-21)15-24(25)27(26)33(19)23-11-9-22(10-12-23)28(2,3)18-29/h4-5,8-17H,1-3H3
• Clave InChI: GVPAGJWVBUZHNQ-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC₅₀ = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC₅₀ = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC₅₀ >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC₅₀ ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70^S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Otras notas

Marone, R., et al. 2009. Mol. Cancer Res.7, 601.
Weisberg, E., et al. 2008. Blood111, 3723.
Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett.18, 1027.

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 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable