ENMD-2076

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ENMD-2076

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Cat No: 22956

Biochemicals - Kinase Inhibitors

ENMD-2076 is a multi-kinase inhibitor that inhibits FMS-related tyrosine kinase 3 (FLT3), RET, and Aurora A kinase with IC50 values of 1.86, 10.4, and 14 nM, respectively.{39604} It inhibits additional kinases involved in angiogenesis such as VEGFR3, ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine, 2R,3R-dihydroxybutanedioate

Correlated keywords:

1291074-87-7 1292319-34-6 934353-76-1 ENMD2076 FLT VEGFR PDGFR-? FGFR-2 multikinase

Product Overview:
ENMD-2076 is a multi-kinase inhibitor that inhibits FMS-related tyrosine kinase 3 (FLT3), RET, and Aurora A kinase with IC50 values of 1.86, 10.4, and 14 nM, respectively.{39604} It inhibits additional kinases involved in angiogenesis such as VEGFR3, PDGFRα, and FGFR2, among others, with IC50 values of less than 100 nM. It inhibits proliferation of several human triple-negative breast cancer (TNBC) cell lines with IC50 values of less than 1 µM, halts the cell cycle at the G2 phase, and induces apoptosis.{39603} Oral administration of ENMD-2076 (200 mg/kg), reduces proliferation, enhances p53- and p73-mediated cancer cell apoptosis and senescence, and inhibits growth of sensitive primary tumors in a TNBC mouse xenograft model.{39605} It also decreases tumor vascular permeability and perfusion and inhibits tumor growth in human TNBC and colorectal cancer mouse xenograft models when administered orally at a dose of 100 mg/kg.{39603,39606}

Size	1 mg
Shipping	dry ice
CAS Number	1453868-32-0
Molecular Formula	C₂₁H₂₅N₇ • C₄H₆O₆
SMILES	CN(CC1)CCN1C2=CC(NC3=NNC(C)=C3)=NC(/C=C/C4=CC=CC=C4)=N2.OC([C@H](O)[C@@H](O)C(O)=O)=O
Molecular Weight	525,6
Formulation	A crystalline solid
Purity	≥98%
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.