1. PI3K/Akt/mTOR
  2. PI3K

NVP-BAG956 (Synonyms: BAG 956)

Cat. No.: HY-13333
Handling Instructions

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

For research use only. We do not sell to patients.

NVP-BAG956 Chemical Structure

NVP-BAG956 Chemical Structure

CAS No. : 853910-02-8

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10 mg USD 380 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

427.50

Formula

C₂₈H₂₁N₅

CAS No.

853910-02-8

SMILES

CC1=NC2=C(C3=CC(C#CC4=CC=CN=C4)=CC=C3N=C2)N1C5=CC=C(C=C5)C(C#N)(C)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NVP-BAG956
Cat. No.:
HY-13333
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NVP-BAG956

Cat. No.: HY-13333