Research Area
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ENMD-2076 Chemical Structure
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Biological Activity
ENMD-2076 is a novel, orally bioavailable multitargeted antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1. ENMD-2076 is relatively selective for the Aurora A isoform in comparison to Aurora B. [1] ENMD-2076 has demonstrated significant, dose-dependent preclinical activity as a single agent, including tumor regression, in multiple xenograft models (e.g. breast, colon, leukemia), as well as activity towards ex vivo-treated human leukemia patient cells. ENMD-2076 is currently in Phase 1 clinical studies in solid tumors and multiple myeloma. ENMD-2076 demonstrated robust antitumor activity against cell line and patient-derived xenograft models of CRC that is detectable by functional imaging, supporting clinical investigation of this agent in human colorectal cancer. [1][2]
References on ENMD-2076
- [1] Clin Cancer Res 2010;16:2989-2998
- [2] Mol Cancer Ther 2011;10:126-137
Chemical Information
| Molecular Weight (WM): | 525.56 |
|---|---|
| Formula: | C25H31N7O6 |
| CAS No.: | 1291074-87-7 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥105mg/mL |
| Water ≥1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Click to enlarge
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.
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.
Data independently produced by Dr Antonino Maria Sparta ,University of Trento ENMD-2076 purchased from Selleck
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Click to enlarge
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.
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.
Data independently produced by Dr Antonino Maria Sparta ,University of Trento ENMD-2076 purchased from Selleck
-
Click to enlarge
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
Data independently produced by Dr Zhang of Tianjin Medical University ENMD-2076 purchased from Selleck
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Click to enlarge
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.
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.
Data independently produced by Dr Antonino Maria Sparta ,University of Trento ENMD-2076 purchased from Selleck
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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.
|
Data independently produced by Dr Antonino Maria Sparta ,University of Trento
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.
|
Data independently produced by Dr Antonino Maria Sparta ,University of Trento
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