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.

• Sinônimo(s): 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 (Notação de Hill): C₂₈H₂₁N₅
• Número CAS: 853910-02-8
• Peso molecular: 427.50
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: orange
• solubilidade: DMSO: 25 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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
• chave InChI: GVPAGJWVBUZHNQ-UHFFFAOYSA-N

Descrição

Descrição geral

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).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras 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.

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