An inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM); selective for these isoforms over the class III PI3K Vps34 (IC50 = 2

NVP-BKM120 – 10 mg

Brand:
Cayman
CAS:
944396-07-0
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (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), PI4Kβ (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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Description

An inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM); selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), mTOR (IC50 = 2,866 nM), PI4Kβ (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM); inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively); crosses the blood brain barrier; increases survival in a U87 glioma mouse xenograft intracranial tumor model when orally administered at 20 and 40 mg/kg once per week

Formal name: 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-pyridinamine

Synonyms:  Buparlisib

Molecular weight: 410.4

CAS: 944396-07-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Transcription Factors|p53

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