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ENMD-2076

Catalog No. T2358 CAS 934353-76-1

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, FLT3, KDR/VEGFR2, FLT4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.

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ENMD-2076, CAS 934353-76-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 47.00
2 mg	In stock	$ 66.00
5 mg	In stock	$ 107.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 293.00
50 mg	In stock	$ 486.00
100 mg	In stock	$ 683.00
1 mL * 10 mM (in DMSO)	In stock	$ 118.00

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Purity: 98%

Purity: 97.63%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
Targets&IC50	FLT3:1.86 nM, Aurora A:14 nM, RET:10.4 nM, Src:20.2 nM, VEGFR3/FLT4:15.9 nM
Kinase Assay	Kinase assays: Recombinant Aurora A and B kinase enzymes and appropriate PanVera Z'-Lyte kinase assay kits are purchased. Assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values. Potency of ENMD-2076 free base against a select panel of 100 kinase enzymes is determined using the SelectScreen kinase profiling service. ATP concentrations are at the apparent Km for each enzyme or 100 μM if the apparent Km could not be reached. Percent inhibition is determined at an ENMD-2076 free base concentration of 1 μM; for kinases where significant inhibition is noted, IC50 values are determined by generating full 10-point dose–response curves.
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)

Molecular Weight	375.47
Formula	C21H25N7
CAS No.	934353-76-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 97 mg/mL (258.3 mM)

H2O: 1 mg/mL (2.66 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Fletcher GC, et al, Mol Cancer Ther, 2011, 10(1), 126-137. 2. Wang X, et al. Br J Haematol, 2010, 150(3), 313-325.

Related compound libraries

This product is contained In the following compound libraries：

Autophagy Compound Library Anti-Fibrosis Compound Library Bioactive Compounds Library Max Clinical Compound Library Osteogenesis Compound Library Orally Active Compound Library Anti-Aging Compound Library Anti-Ovarian Cancer Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ENMD-2076 934353-76-1 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR Src c-RET FLT Aurora Kinase Cluster of differentiation antigen 135 FLT3 Inhibitor Fibroblast growth factor receptor CD135 Platelet-derived growth factor receptor ENMD 2076 Vascular endothelial growth factor receptor Fms like tyrosine kinase 3 ENMD2076 inhibit inhibitor

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