A multi-kinase inhibitor; inhibits FLT3

ENMD-2076 – 10 mg

Brand:
Cayman
CAS:
934353-76-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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}  

 

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SKU: 22956 - 10 mg Category:

Description

A multi-kinase inhibitor; inhibits FLT3, RET, and Aurora A kinase (IC50s = 1.86, 10.4, and 14 nM, respectively); inhibits additional kinases involved in angiogenesis (IC50s = 50s = via oral gavage); decreases tumor vascular permeability and perfusion and inhibits tumor growth in human TNBC and colorectal cancer mouse xenograft models of (100 mg/kg via oral gavage)

Formal name: 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine

Synonyms: 

Molecular weight: 375.5

CAS: 934353-76-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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