NVP-BKM120

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NVP-BKM120

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Cat No: 11587

Biochemicals - Kinase Inhibitors

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 (m...

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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 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}

Size	1 mg
Shipping	dry ice
CAS Number	944396-07-0
Molecular Formula	C₁₈H₂₁F₃N₆O₂
SMILES	NC(N=C1)=CC(C(F)(F)F)=C1C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2
Molecular Weight	410,4
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2933.59
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.