ENMD-2076

• CAT Number: I006675
• CAS Number: 934353-76-1
• Molecular Formula: C₂₁H₂₅N₇
• Molecular Weight: 375.47
• Purity: ≥95%
• Synonyms: ENMD2076; ENMD 2076; ENMD-2076.;(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine.
• Target: Aurora Kinase; FLT3; VEGFR; FGFR; PDGFR; Src; Apoptosis
• Solubility: Soluble in DMSO, not in water
• Storage: 3 years -20C powder
• Related CAS: 1291074-87-7 (tartrate)
• IUPAC Name: 6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine
• InChI: InChI=1S/C21H25N7/c1-16-14-20(26-25-16)23-19-15-21(28-12-10-27(2)11-13-28)24-18(22-19)9-8-17-6-4-3-5-7-17/h3-9,14-15H,10-13H2,1-2H3,(H2,22,23,24,25,26)/b9-8+
• InChIKey: BLQYVHBZHAISJM-CMDGGOBGSA-N
• SMILES: CC1=CC(=NN1)NC2=CC(=NC(=N2)/C=C/C3=CC=CC=C3)N4CCN(CC4)C

ENMD-2076（Cat No.:I006675）is a small molecule inhibitor that selectively targets the tyrosine kinase pathways involved in tumor growth and angiogenesis. Specifically, it inhibits the activity of multiple kinases, including the vascular endothelial growth factor receptor (VEGFR) and the fibroblast growth factor receptor (FGFR). By disrupting these signaling pathways, ENMD-2076 exhibits antitumor activity, making it a candidate for treating various cancers, particularly solid tumors. Preclinical studies and early-phase clinical trials have demonstrated its potential efficacy and safety profile, with ongoing research focused on optimizing its use in combination with other therapies.

Reference

1:A phase I trial of the aurora kinase inhibitor, ENMD-2076, in patients with relapsed or refractory acute myeloid leukemia or chronic myelomonocytic leukemia. Yee KW, Chen HW, Hedley DW, Chow S, Brandwein J, Schuh AC, Schimmer AD, Gupta V, Sanfelice D, Johnson T, Le LW, Arnott J, Bray MR, Sidor C, Minden MD.Invest New Drugs. 2016 Oct;34(5):614-24. doi: 10.1007/s10637-016-0375-2. Epub 2016 Jul 12. PMID: 27406088
2:The radiosensitizing effect of the aurora kinase inhibitors, ENMD-2076, on canine mast cell tumours in vitro. Shiomitsu K, Sajo E, Rubin C, Sehgal I.Vet Comp Oncol. 2016 Mar;14(1):13-27. doi: 10.1111/vco.12046. Epub 2013 Jun 13. PMID: 23763774 Free PMC Article
3:Predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor ENMD-2076 in preclinical breast cancer models. 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.Clin Cancer Res. 2013 Jan 1;19(1):291-303. doi: 10.1158/1078-0432.CCR-12-1611. Epub 2012 Nov 7. PMID: 23136197 Free PMC Article
4:[Killing effect of aurora kinase inhibitor ENMD-2076 on acute myelogenous leukemia cells]. Cao H, Li M, Qian WB.Zhejiang Da Xue Xue Bao Yi Xue Ban. 2012 Sep;41(5):479-84. Chinese. PMID: 23086638
5:ENMD-2076, an oral inhibitor of angiogenic and proliferation kinases, has activity in recurrent, platinum resistant ovarian cancer. Matulonis UA, Lee J, Lasonde B, Tew WP, Yehwalashet A, Matei D, Behbakht K, Grothusen J, Fleming G, Lee NK, Arnott J, Bray MR, Fletcher G, Brokx RD, Castonguay V, Mackay H, Sidor CF, Oza AM.Eur J Cancer. 2013 Jan;49(1):121-31. doi: 10.1016/j.ejca.2012.07.020. Epub 2012 Aug 21. PMID: 22921155
6:ENMD-2076 for hematological malignancies. How J, Yee K.Expert Opin Investig Drugs. 2012 May;21(5):717-32. doi: 10.1517/13543784.2012.668882. Epub 2012 Mar 8. Review. PMID: 22397360
7:From cell biology to therapy: ENMD-2076 in the treatment of multiple myeloma. Zhang S, Farag SS.Expert Opin Investig Drugs. 2011 Jul;20(7):1015-28. doi: 10.1517/13543784.2011.584869. Epub 2011 May 26. Review. PMID: 21615212
8:ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Fletcher GC, Brokx RD, Denny TA, Hembrough TA, Plum SM, Fogler WE, Sidor CF, Bray MR.Mol Cancer Ther. 2011 Jan;10(1):126-37. doi: 10.1158/1535-7163.MCT-10-0574. Epub 2010 Dec 21. PMID: 21177375 Free Article
9:Phase I safety, pharmacokinetic, and pharmacodynamic study of ENMD-2076, a novel angiogenic and Aurora kinase inhibitor, in patients with advanced solid tumors. Diamond JR, Bastos BR, Hansen RJ, Gustafson DL, Eckhardt SG, Kwak EL, Pandya SS, Fletcher GC, Pitts TM, Kulikowski GN, Morrow M, Arnott J, Bray MR, Sidor C, Messersmith W, Shapiro GI.Clin Cancer Res. 2011 Feb 15;17(4):849-60. doi: 10.1158/1078-0432.CCR-10-2144. Epub 2010 Dec 3. PMID: 21131552 Free PMC Article
10:Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Wang X, Sinn AL, Pollok K, Sandusky G, Zhang S, Chen L, Liang J, Crean CD, Suvannasankha A, Abonour R, Sidor C, Bray MR, Farag SS.Br J Haematol. 2010 Aug;150(3):313-25. doi: 10.1111/j.1365-2141.2010.08248.x. Epub 2010 Jun 15. PMID: 20560971