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NVP-BAG956

Catalog No. TQ0313 CAS 853910-02-8

Synonyms: BAG956

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

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NVP-BAG956, CAS 853910-02-8

Pack Size	Availability	Price/USD	Quantity
50 mg	6-8 weeks	$ 747.00
100 mg	6-8 weeks	$ 1,360.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NVP-BAG956 is an ATP-competitive PI3K inhibitor (IC50s: 34/56/112/444 nM for PI3Kδ/PI3Kα/PI3Kγ/PI3Kβ).
Targets&IC50	PI3Kγ:117 nM, PDK1:240 nM, PI3Kα:56 nM, PI3Kβ:446 nM, PI3Kδ:35 nM, VEGFR1:2.56 μM
In vitro	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.
Cell Research	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.

Synonyms	BAG956
Molecular Weight	427.5
Formula	C28H21N5
CAS No.	853910-02-8

Storage

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

Solubility Information

DMSO: Soluble

References and Literature

1. Marone R, et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13.

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Keywords

NVP-BAG956 853910-02-8 PI3K/Akt/mTOR signaling PI3K NVP BAG956 NVPBAG956 BAG-956 NVP-BAG-956 BAG 956 NVP-BAG 956 BAG956 inhibitor inhibit

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