CH5132799

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CH5132799

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Cat No: 26410

Biochemicals - Kinase Inhibitors

CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2α and PI3KC2β, which are class II PI3Ks, Vps34, a class II...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-pyrimidinamine

Correlated keywords:

1431855-32-1 CH-5132799 5137291 PA799 PI3K-? ?H1047R ? ? ? C2? C2? Vps-34 HCT-116 KPL4 T-47D SKOV-3 PC-3 PA-799 CH5137291

Product Overview:
CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2α and PI3KC2β, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3KαH1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.

Size	5 mg
Shipping	dry ice
CAS Number	1007207-67-1
Molecular Formula	C₁₅H₁₉N₇O₃S
SMILES	NC(N=C1)=NC=C1C2=NC(N3CCOCC3)=NC4=C2CCN4S(C)(=O)=O
Molecular Weight	377,4
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.