ENMD-2076 Tartrate

• CAT Number: I001126
• CAS Number: 1291074-87-7
• Molecular Formula: C25H31N7O6
• Molecular Weight: 525.56
• Purity: ≥95%
• Synonyms: (E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine 2,3-dihydroxysuccinate
• Target: Aurora Kinase; FLT3; VEGFR; FGFR; Src; PDGFR; Apoptosis
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 14 nM (Aurora A); 1.86 nM (Flt3); 58.2 nM (VEGFR2)
• IUPAC Name: (2S,3S)-2,3-dihydroxybutanedioic acid;6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine
• InChI: InChI=1S/C21H25N7.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h3-9,14-15H,10-13H2,1-2H3,(H2,22,23,24,25,26);1-2,5-6H,(H,7,8)(H,9,10)/b9-8+;/t;1-,2-/m.0/s1
• InChIKey: KGWWHPZQLVVAPT-PCWHHUEVSA-N
• SMILES: CC1=CC(=NN1)NC2=CC(=NC(=N2)/C=C/C3=CC=CC=C3)N4CCN(CC4)C.[C@H]([C@@H](C(=O)O)O)(C(=O)O)O

ENMD-2076 Tartrate (Cat No.:I001126) is a small-molecule kinase inhibitor with potential anti-cancer activity. It targets multiple kinases, including Aurora A, Flt3, VEGFR2, FGFR3, and Src, among others. ENMD-2076 exhibits inhibitory effects on angiogenesis and tumor growth in preclinical studies. It has shown activity against a wide range of cancer types, including ovarian, breast, colorectal, and multiple myeloma. ENMD-2076 has been investigated in clinical trials for various malignancies, both as a single agent and in combination with other therapies. It holds promise as a targeted therapeutic option for cancer treatment, particularly in patients with advanced or refractory disease.

Reference

[1]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative 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.