Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :ENMD-2076 Tartrate1291074-87-7HY-10987525.56C25H31N7O6>98%ySolubility:DMSOMechanisms: Pathways:Cell Cycle/DNA Damage; Target:Aurora Kinase Pathways:Protein Tyrosine Kinase/RTK; Target:FLT3 Pathways:Protein Tyrosine Kinase/RTK; Target:VEGFR Biological Activity:ENMD-2076 tartrate has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86ENMD2076tartratehasselectiveactivityagainstAuroraAandFlt3withIC50of14nMand186nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR andVEGFR3, FGFR1 and FGFR2 and PDGFRα. IC50 value: 14 nM (Aurora A); 1.86 nM (Flt3); 58.2 nM (VEGFR2) [1] Target: Flt3; Aurora A in vitro: ENMD-2076 indicates activity against multiple kinases involved in angiogenesis, includingFLT3, RET, FLT4/VEGFR3, SRC, NTRK1, CSF1R/FMS, LCK, VEGFR2/KDR, FGFR1/2, andPDGFRα with IC50 from 1.86-120 nM. ENMD-2076 inhibits the growth of a wide range of humanpμM, which induces,solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 apoptosis and G2/M phase arrest. ENMD-2076 induces regression or complete inhibition of tumorgrowth in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiplemyeloma cell lines [1...References:[1]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic andantiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37. [2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor,ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com 18 Wilkinson Way, Princeton, NJ 080,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
