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

Description

ENMD-2076 (Tartrate) is a multi-targeted antiangiogenic and Aurora kinase inhibitor with potent inhibitory effects on various kinases, including Flt-3, AurA, AurB, Src, KDR/VEGFR2, and FGFR1. It is a promising pharmaceutical candidate for the treatment of various diseases, particularly those involving abnormal cell proliferation and angiogenesis.

Uses

Used in Oncology:
ENMD-2076 (Tartrate) is used as an antiangiogenic agent for the inhibition of blood vessel formation in tumors, thereby limiting their growth and progression. It targets multiple kinases, such as Flt-3, KDR/VEGFR2, and FGFR1, which play crucial roles in angiogenesis and tumor development.
Additionally, ENMD-2076 (Tartrate) is used as an Aurora kinase inhibitor for the suppression of abnormal cell division and proliferation. It inhibits AurA, AurB, and Src kinases, which are involved in cell cycle regulation and are often dysregulated in cancer cells.

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.