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.

• 동의어(들): 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
• 실험식(Hill 표기법): C₂₈H₂₁N₅
• CAS Number: 853910-02-8
• Molecular Weight: 427.50
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: orange
• solubility: DMSO: 25 mg/mL
• 배송 상태: ambient
• 저장 온도: 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

설명

일반 설명

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).

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable