GSK2126458

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GSK2126458

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Cat No: 17377

Biochemicals - Kinase Inhibitors

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively).{20675} It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-benzenesulfonamide

Correlated keywords:

GSK-2126458 458 mTORC-1 2 p110a b d g anti-tumor SNU1040 DDR 1 DDR1IN1

Product Overview:
GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively).{20675} It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110α.{20675} GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models.{20675} GSK2126458 positively combines with inhibitors of discoidin domain receptor 1 (DDR1) inhibitor DDR1-IN-1 (Item No. 18092) to suppress the growth of SNU-1040 colorectal cancer cells.{29876}

Size	1 mg
Shipping	dry ice
CAS Number	1086062-66-9
Molecular Formula	C₂₅H₁₇F₂N₅O₃S
SMILES	COC1=C(NS(C2=CC=C(F)C=C2F)(=O)=O)C=C(C3=CC(C(C4=CC=NN=C4)=CC=N5)=C5C=C3)C=N1
Molecular Weight	505,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

Technical File

MSDS

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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.