ENMD-2076

SKU: orb1305600

Description

ENMD-2076

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 934353-76-1
• MW: 375.47
• Purity: ≥95%
• Formula: C₂₁H₂₅N₇
• SMILES: CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(\C=C\c2ccccc2)n1
• Target: Src,Aurora Kinase,FLT,c-RET,VEGFR,PDGFR,Apoptosis,FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.79 mM);DMSO:97 mg/mL (258.34 mM);H2O:1 mg/mL (2.66 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  KDR:58.2 nM|Aurora A:14 nM|FGFR1:92.7 nM|PDGFRα:56.4 nM|FLT3:1.86 nM|FGFR2:70.8 nM|VEGFR3/FLT4:15.9 nM|RET:10.4 nM|Src:20.2 nM
• In Vivo:
  ENMD-2076 targets the PI3K/AKT pathway, leading to the downregulation of apoptosis-inhibiting proteins. It inhibits aurora kinases A and B, causing cell cycle arrest at the G2/M phase. ENMD-2076 is effective against various angiogenesis-related kinases (IC50=1.86-120 nM), including VEGFR2/KDR, VEGFR3, FGFR1, FGFR2, and PDGFRα. In multiple human solid tumor and leukemia cell lines (IC50=0.025-0.7 μM), it induces cell cycle arrest at the G2/M phase and promotes apoptosis.
• In Vitro:
  In the MDA-MB-231 xenograft model, ENMD-2076 was observed to inhibit neovascularization while also inducing regression in already formed vessels. Within the HT29 xenograft model, ENMD-2076 consistently inhibited the activation of Flt3, as well as VEGFR2 / KDR and FGFR1 / 2. In the case of H929 human myeloma xenografts, oral administration of ENMD-2076 (50-200 mg/kg/day) resulted in a significant decrease in phospho-histone 3 (pH3) and Ki-67, alongside a notable increase in cleaved caspase-3, indicating effective antitumor activity through inhibition of cell proliferation and induction of apoptosis.
• Cell Research:
  The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with ENMD-2076 for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay. The leukemia-derived, nonadherent cell lines are assayed by plating 5 × 103 cells per well in a 96-well plate. The cells are incubated with ENMD-2076 for 48 hours and then survival is assayed using the Alamar Blue reagent. To measure the effect of ENMD-2076 on VEGF- and fibroblast growth factor (FGF)-induced proliferation of human umbilical vein endothelial cell (HUVEC), cells are serum starved for 6 hours, then treated with ENMD-2076 free base, and stimulated with 5 ng/mL bFGF or 25 ng/mL VEGF (R and D Systems) for 72 hours. Cell proliferation is measured using WST-(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Src, RET, PDGFR, VEGFR, VEGFR3/FLT4, Vascular endothelial growth factor receptor, ENMD 2076, ENMD2076, ENMD-2076, Fms like tyrosine kinase 3, Fibroblast growth factor receptor, FGFR, FLT3, Inhibitor, inhibit, Platelet-derived growth factor receptor, CD135, Cluster of differentiation antigen 135, cRET, AuroraKinase, Aurora Kinase, Aurora A, Apoptosis

Compound Identifiers

PubChem CID

16041424