NVP-<wbr/>BKM120

NVP-BKM120

CAT N°: 11587
Price:

From €48.00 €40.80

NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110? (IC50 = 52 nM) and p110? (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4K? (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-pyridinamine
  • Correlated keywords
    • Inhibitors signals transductions cancers inhibitions inhibits PI3K phosphatidylinositol 3-kinases 3 kinases BKM-120 BKM 120 class I isoforms III cancers cells lines tumors growths in vivo modulators bioavailables orally signals transductions lipids NVP-BKM120 NVP blocking p110? p110? p110 alpha beta Vps34 Vps 34 mTOR PI4K? P14K prevents vitro
  • Product Overview:
    NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110? (IC50 = 52 nM) and p110? (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4K? (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}

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