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AZD1480

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    AZD1480
  • AZD1480
Cat No: 10702
Biochemicals - Kinase Inhibitors
Cayman
€38.00
Price is excluding VAT and does not include packaging neither shipping

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch fro...

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Territorial Availability: Available through Bertin Pharma only in Europe
Synonyms:
  • 5-chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
Correlated keywords:
  • JAK2 JAK 2 STAT3 STAT 3 STAT5 STAT 5 AZD 1480 janus-associated kinase
Product Overview:
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}
Size 1 mg
Shipping dry ice
Stability Store at -20 degrees; shelf life 730 days
CAS Number 935666-88-9
Molecular Formula C14H14ClFN8
SMILES ClC1=C(NC2=NNC(C)=C2)N=C(N[C@@H](C)C3=NC=C(F)C=N3)N=C1
Molecular Weight 348,8
Formulation A crystalline solid
Purity ≥98%
Custom Code 2903.99
UNSPSC code 12352100

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.

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