1291074-87-7

Basic information

• Product Name: ENMD-2076 (Tartrate)
• Synonyms: (E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine,L-(+)-Tartaric acid;ENMD-2076 (Tartrate);ENMD-2076 L-(+)-Tartaric acid
• CAS NO: 1291074-87-7
• Molecular Formula: C21H25N7.x(C4H6O6)
• Product Categories: Inhibitors;Inhibitor
• Mol File: 1291074-87-7.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Solubility: insoluble in EtOH; ≥175.8 mg/mL in DMSO
• CAS DataBase Reference: ENMD-2076 (Tartrate)(CAS DataBase Reference)
• NIST Chemistry Reference: ENMD-2076 (Tartrate)(1291074-87-7)
• EPA Substance Registry System: ENMD-2076 (Tartrate)(1291074-87-7)

Safety Data

• Hazardous Substances Data: 1291074-87-7(Hazardous Substances Data)

Usage

Uses

ENMD-2076 (ENMD-981693, ENMD2076) is a antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1.

Biological Activity

enmd-2076 is an orally bioavailable, small molecule inhibitor of aurora kinases with ic50 values of 14nm and 350nm, respectively against aurora kinase a and aurora kinase b [1].besides aurora kinases, enmd-2076 inhibits multiple kinases involved in various cellular activities. overexpression of aurora kinase a has been found in breast cancers and enmd-2076 is thereby studied in breast cancers. it is reported that enmd-2076 differentially inhibits 29 breast cancer cell lines with ic50 values ranged from 0.25 to 16.1μm. in the clonogenic assays, enmd-2076 totally suppresses the colony formation in the sensitivemda-mb-468 cell line and decreases the formation in thehcc1806, sk-br-3, and bt474 cell lines. enmd-2076 is also reported to cause a g2 cell-cycle arrest at 1.25μm. moreover, enmd-2076 shows antitumor activity in tnbc xenograft models. apart from the breast cancers, enmd-2076 is developed in hematological malignancies therapy. the

references

[1] diamond jr, eckhardt sg, tan ac, newton tp, selby hm, brunkow kl, kachaeva mi, varella-garcia m, pitts tm, bray mr, fletcher gc, tentler jj. predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor enmd-2076 in preclinical breast cancer models. clin cancer res. 2013 jan 1;19(1):291-303. [2] how j, yee k. enmd-2076 for hematological malignancies. expert opin investig drugs. 2012 may;21(5):717-32.