ENMD-2076

ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Product Specifications

CAS Number

[934353-76-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Aurora Kinase; FGFR; FLT3; PDGFR; Src; VEGFR

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/enmd-2076.html

Purity

99.99

Solubility

DMSO : ≥ 31 mg/mL

Smiles

CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1

Molecular Formula

C21H25N7

Molecular Weight

375.47

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

Aurora A; PDGFRα; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

Citation 01

Am J Pathol. 2019 Oct;189 (10) :2090-2101.|Int J Gynecol Cancer. 2017 Oct;27 (8) :1666-1674. |Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Am J Pathol. 2019 Oct;189 (10) :2090-2101.