Molecular Weight(MW): 375.47
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
4 Customer Reviews
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
Dr. Zhang of Tianjin Medical University. ENMD-2076 purchased from Selleck.
ENMD-2076 has benn tested it on two different neurobiastoma cell lines(SK-N-BE(2) and CHP-134),being calculated the IC50 by a WST-1(Roche) proliferation assay, as shown in the table below. Its in vitro activity is in the micromolar range and has a comparable effect on both lines.VX-680 was used as standard, and it proved more potent on CHP-134 cells.
Dr. Antonino Maria Sparta ,University of Trento. ENMD-2076 purchased from Selleck.
Neurospheres were obtained growing CHP-134 cells in a selective medium (DMEMF12, B27, EGF, bFGF, L-Glut). The cells were grown in 96-well plates to confluence and treated with ENMD-2076 for 24 h. The toxic effect was measured by a WST-1 chromogenic assay. It appears that the bulk cell line is more sensitive to treatment that the neurospheres.
Dr. Antonino Maria Sparta ,University of Trento. ENMD-2076 purchased from Selleck.
SDS-PAGE of CHP-134 cells extracts after 24 h exposure to the indicated drug and concentration. N-myc levels were evaluated and compared to beta actin used as house-keeping protein. Aurora A blockade seems to diminish N-myc expression or stability.
Dr. Antonino Maria Sparta, University of Trento. ENMD-2076 purchased from Selleck.
Purity & Quality Control
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|Description||ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.|
|Features||Multi-target, anti-proliferative, pro-apoptotic activity, anti-angiogenic.|
ENMD-2076 indicates activity against multiple kinases involved in angiogenesis, including FLT3, RET, FLT4/VEGFR3, SRC, NTRK1, CSF1R/FMS, LCK, VEGFR2/KDR, FGFR1/2, and PDGFRα with IC50 from 1.86-120 nM. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. ENMD-2076 induces regression or complete inhibition of tumor growth in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines.  ENMD-2076 is the L (+) tartrate salt of ENMD-981693. ENMD-2076 shows significant cytotoxicity against myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells with IC50 from 2.99 to 7.06 μM, which induces apoptosis. ENMD-2076 indicates low cytotoxicity to haematopoietic progenitors. ENMD-2076 inhibits the phosphoinositide 3-kinase/Akt pathway and downregulates survivin and X-linked inhibitor of apoptosis. ENMD-2076 also inhibits aurora A and B kinases, and induces G2/M cell cycle arrest. 
|In vivo||ENMD-2076 has sustained inhibitory effects on the activation of Flt3 as well as VEGFR2/KDR and FGFR1/2 in HT29 xenograft model. ENMD-2076 could prevent the formation of new blood vessels and regress formed vessels in MDA-MB-231 xenograft model.  Oral treatment with ENMD-2076 (50, 100, 200 mg/kg per day) inhibits the tumour growth in H929 human plasmacytoma xenografts, with significant reduction in phospho-Histone 3 (pH3), Ki-67, and angiogenesis, and also a significant increase in cleaved caspase-3. |
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.
|In vitro||DMSO||105 mg/mL (279.64 mM)|
|Water||1 mg/mL (2.66 mM)|
|In vivo||0.5% CMC+0.25% Tween 80||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02234986||Recruiting||Advanced Adult Hepatocellular Carcinoma|Advanced Fibrolamellar Carcinoma||CASI Pharmaceuticals, Inc.||October 2015||Phase 2|
|NCT01914510||Recruiting||Ovarian Clear Cell Carcinoma||University Health Network, Toronto||September 2013||Phase 2|
|NCT01719744||Completed||Advanced|Metastatic|Soft Tissue Sarcoma||University Health Network, Toronto||January 2013||Phase 2|
|NCT01639248||Recruiting||Triple Negative Breast Cancer||CASI Pharmaceuticals, Inc.|University of Colorado, Denver|Indiana University Melvin and Bren Simon Cancer Center||July 2012||Phase 2|
|NCT01104675||Completed||Ovarian Cancer|Fallopian Cancer|Peritoneal Cancer||CASI Pharmaceuticals, Inc.||April 2010||Phase 2|
|NCT00904787||Completed||Relapsed or Refractory Hematological Malignancies||CASI Pharmaceuticals, Inc.||April 2009||Phase 1|
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