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BKM120 (NVP-BKM120)

Catalog No.S2247 1 Review(s)
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BKM120 (NVP-BKM120) Chemical Structure

  • BEZ235 (NVP-BEZ235)

    BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.

  • Perifosine

    Perifosine is an Akt inhibitor. the antiproliferative properties of perifosine with an IC50 of 0.6–8.9 µM.

  • PI-103

    PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.

  • GDC-0941

    Inhibitor of Class I PI3 Kinase,p110a IC50=0.003uM,U87MG IC50=0.95μM.

  • ZSTK474

    ZSTK474 is an inhibitor of PI3K γ(IC50 at 6 nM).

  • LY294002

    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.

  • XL147

    XL147 is a selective inhibitor of Class I PI3K isoforms.

  • TGX-221

    TGX-221 is a low-nanomolar range PI3Kβ inhibitor (IC50=10nM), shows about 1000-fold higher selectivity over PI3Kα, and is cell permeable. Order TGX-221 from supplier Selleck for research use only.

  • PIK-90

    PIK-90 is a PI3K inhibitor,IC50=11, 350, 18, and 58 for p110 α, β, γ and δ isoforms.

  • PIK-75

    PIK-75 Hydrochloride is a hydrochloride salt form of PIK-75, which is a preferential p110α/γ forms of PI3K inhibitor with IC50 of 6, 1300, 76, 510 nM for p110α, p110β, p110γ, p110δ, respectively.

Biological Activity

BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor. BKM120 inhibits tumor proliferation and survival by blocking the phosphatidylinositol-3-kinase (PI3K) pathway. BKM120 has shown significant cell growth inhibition and induction of apoptosis in a variety of tumor cell lines as well as in animal models. BKM120 specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. [1][2][3]

References on BKM120 (NVP-BKM120)
  • [] Oncotarge 2010 September 1;1(5): 339–348
Molecular Weight (WM): 410.39
Formula:

C18H21F3N6O2

CAS No.: 944396-07-0
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥82mg/mL 
Water <1mg/mL 
Ethanol ≥25mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

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    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of BKM120 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of BKM120 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • Data independently produced by Dr. Zhang of Tianjin Medical University
    BKM120 (NVP-BKM120) purchased from Selleck

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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of BKM120 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

Data independently produced by Dr. Zhang of Tianjin Medical University

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