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Angiogenesis FLT ENMD2076

ENMD2076

Catalog No. T2358   CAS 934353-76-1
Synonyms: ENMD 2076, ENMD-2076

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.

ENMD2076, CAS 934353-76-1
Pack Size Availability Price/USD Quantity
2 mg In stock 74.00
5 mg In stock 120.00
10 mg In stock 180.00
25 mg In stock 446.00
50 mg In stock 540.00
100 mg In stock 760.00
1 mL * 10 mM (in DMSO) In stock 136.00
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Purity 97.63%
Purity 98.00%
Purity 98.00%
Biological Description
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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 Aurora A : ic50 14nM ,   FLT3 : ic50 1.86nM ,   RET : ic50 10.4nM ,   Src : ic50 20.2nM ,   VEGFR3/FLT4 : ic50 15.9nM
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)
Cell lines: Human leukemia cell lines including MV4;11, U937, Kasumi, MO7e, HL-60, TF-1, Jurkat, K562, THP-1, Hel 92.1.7; Solid tumor cell lines and HUVEC including PANC-1, HCT116, A549, HT-29, MCF7, PC-3, BXPC-3 and HUVEC
Animal Research
Animal Model: Tumor models including HCT-116, HT29, CT-26, A375, MDA-MB-231, H929, OPM-2, MV4;11 and HL60 are established in CB.17 SCID or NCr nude mice.
Synonyms ENMD 2076 , ENMD-2076
Purity 97.63%
Molecular Weight 375.47
Formula C21H25N7
CAS No. 934353-76-1

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 97 mg/mL (258.3 mM)

Water: 1 mg/mL (2.66 mM)

Ethanol: <1 mg/mL

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

Solution 1

0.5% CMC+0.25% Tween 80: 30 mg/mL

Citations

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:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Apoptosis Compound Library Autophagy Compound Library Epigenetics Compound Library Tyrosine kinase inhibitor library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library Cell cycle related Compound Library

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