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NVP-BAG956

Names

[ CAS No. ]:
853910-02-8

[ Name ]:
NVP-BAG956

[Synonym ]:
cc-502
BAG956
2-Methyl-2-(4-(2-methyl-8-((pyridin-3-yl)ethynyl)imidazo(4,5-C)quinolin-1-yl)phenyl)propionitrile
Benzeneacetonitrile, α,α-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-
2-Methyl-2-{4-[2-methyl-8-(pyridin-3-ylethynyl)-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
2-Methyl-2-{4-[2-methyl-8-(3-pyridinylethynyl)-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
NVP-BAG956
UNII-4UFC2K6E50

Biological Activity

[Description]:

NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Research Areas >> Cancer

[Target]

PI3Kδ:35 nM (IC50)

PI3Kα:56 nM (IC50)

PI3Kγ:117 nM (IC50)

PI3Kβ:446 nM (IC50)

PDK1:240 nM (IC50)

VEGFR1:2.56 μM (IC50)


[In Vitro]

NVP-BAG956 also inhibits PDK1 with an IC50 of 240/260 nM. NVP-BAG956 also inhibits VEGFR1 with an IC50 of 2.56±0.56 μM. NVP-BAG956 blocks phosphorylation of PKB/Akt in A2058 cells with an IC50 value of 67±25 nM. Inhibition of PKB/Akt phosphorylation correlated with loss of A2058 cell proliferation for NVP-BAG956 (IC50=290±20 nM). In the presence of NVP-BAG956, A2058 cells are only able to exit G2-M and then remain in G1. The p27 Kip1 expression is clearly induced by NVP-BAG956 in A2058 cells but not in C32 cells[1].

[Cell Assay]

One day after plating (7×103 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[1].

[References]

[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.


[Related Small Molecules]

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | 740 Y-P | LY3023414 | 1,3-Dicaffeoylquinic acid

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
694.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H21N5

[ Molecular Weight ]:
427.500

[ Flash Point ]:
374.0±34.3 °C

[ Exact Mass ]:
427.179688

[ PSA ]:
67.39000

[ LogP ]:
4.75

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.655

[ Storage condition ]:
-20℃

Related Compounds