化合物NVP-BAG956 TQ0313

Product Introduction
Bioactivity


英文名: NVP-BAG956

描述: NVP-BAG956 is an ATP-competitive PI3K inhibitor (IC50s: 34/56/112/444 nM for PI3Kδ/PI3Kα/PI3Kγ/PI3Kβ).

细胞实验: One day after plating (7×10^3 cells/cm2), melanoma cells (A2058, B16F1, B16F10, C32, HBL, Malme, Malme3M, NA8, SKMel2, SKMel23, A375, Hs294T, WM35, and 1205lu cells) are exposed to LY294002 (25 μM), Wortmannin (500 nM), NVP-BAG956 (1 μM), NVP-BBD130 (1 μM), NVP-BEZ235 (1 μM), and ZSTK474 (1 μM), and Rapamycin (100 nM). Compound concentrations are set 2 log units above the IC50 in vitro to ensure full PI3K inhibition, except for the μM inhibitor LY294002. Cells are trypsinized and counted, and the volume is quantified using a Casy Counter and Analyser. To determine the nuclear volume, cells are resuspended in CASYton containing 0.5% Triton X-100, followed by repetitive pipetting (8×), before volume measurements.

体外活性: NVP-BAG956 also inhibits PDK1 (IC50: 240 nM) and VEGFR1 (IC50: 2.56 μM). NVP-BAG956 blocks phosphorylation of PKB/Akt in A2058 cells (IC50: 67 nM). Inhibition of PKB/Akt phosphorylation correlated with loss of A2058 cell proliferation for NVP-BAG956 (IC50: 290 nM). In the presence of NVP-BAG956, A2058 cells are only able to exit G2-M and then remain in G1. The p27Kip1 expression is clearly induced by NVP-BAG956 in A2058 cells but not in C32 cells.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : Soluble


关键字: NVP BAG956 | NVPBAG956 | BAG-956 | NVP-BAG956 | NVP-BAG-956 | BAG 956 | NVP-BAG 956

相关产品: AMG 511 | PI3Kα/mTOR-IN-1 | PI3K-IN-41 | Hirsutenone | Umbralisib | PI3K-IN-9 | PI4KIIIbeta-IN-9 | (2S,3R,4S)-4-Hydroxyisoleucine | Autophinib | RLY-2608

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途