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
