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.

• 別名: 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
• 実験式（ヒル表記法）: C₂₈H₂₁N₅
• CAS番号: 853910-02-8
• 分子量: 427.50
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 25 mg/mL
• 輸送温度: ambient
• 保管温度: 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
• InChI Key: GVPAGJWVBUZHNQ-UHFFFAOYSA-N

詳細

詳細

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).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable