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Chemical Structure| 934353-76-1 Chemical Structure| 934353-76-1

Structure of ENMD-2076
CAS No.: 934353-76-1

Chemical Structure| 934353-76-1

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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.

Synonyms: ENMD-2076

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Product Details of ENMD-2076

CAS No. :934353-76-1
Formula : C21H25N7
M.W : 375.47
SMILES Code : CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1
Synonyms :
ENMD-2076
MDL No. :MFCD16619371

Safety of ENMD-2076

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of ENMD-2076

epigenetics
DNA
RTK

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, IC50:14 nM

  • Aurora B

    Aurora B, IC50:350 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:15.9 nM

  • VEGFR2

    VEGFR2/KDR, IC50:58.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HL-7702 0.5, 1, 5μM 24, 48, 72 h ENMD-2076 possessed limited toxicity to normal cells PMC6874459
C6 0, 0.5, 1, 2, 4, 8μM 24, 48, 72 h ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner PMC6874459
U251 0, 0.5, 1, 2, 4, 8μM 24, 48, 72 h ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner PMC6874459
U87 0, 0.5, 1, 2, 4, 8μM 24, 48, 72 h ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner PMC6874459
T98G 0, 0.5, 1, 2, 4, 8μM 24, 48, 72 h ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner PMC6874459
LN18 0, 0.5, 1, 2, 4, 8μM 24, 48, 72 h ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner PMC6874459
MDA-MB-468 0 – 5 μM 96 h To evaluate the effect of ENMD-2076 on DNA synthesis PMC3537923
HCC1143 0 – 20 μM 24 -96 h To evaluate the antiproliferative activity of ENMD-2076 against breast cancer cell lines PMC3537923
VI-MC1 291 nM (IC10), 539 nM (IC50) 48 h Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells PMC3812382
CM-MC1 17.5 nM (IC10), 404 nM (IC50) 48 h Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity PMC3812382
CoMS 117 nM (IC10), 360 nM (IC50) 48 h Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells PMC3812382

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Intracranial tumor model Oral 50 mg/kg, 200 mg/kg 28 days ENMD-2076 significantly prolonged the survival time of tumor-bearing rats as well as inhibiting tumor growth (p<0.01) PMC6874459
Nude mice MDA-MB-468 and MDA-MB-231 triple-negative breast cancer xenografts Oral gavage 100 mg/kg Once daily for 16 days (MDA-MB-231) or 40 days (MDA-MB-468) To evaluate the antitumor activity of ENMD-2076 in triple-negative breast cancer xenograft models PMC3537923
Nude mice HT-29 CRC cell line xenograft model Oral 100 or 200 mg/kg Daily for 28 days To evaluate the antitumor effects of ENMD-2076 on HT-29 CRC xenograft models. Results showed that ENMD-2076 at doses of 100 and 200 mg/kg significantly inhibited tumor growth and reduced tumor vascularity and metabolic activity. PMC3928713

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01914510 Ovarian Clear Cell Carcinoma PHASE2 COMPLETED 2025-01-17 Tom Baker Cancer Centre, Calga... More >>ry, Alberta, T2N 4N2, Canada|Cross Cancer Institute, Edmonton, Alberta, T6G 1Z2, Canada|British Columbia Cancer Agency, Vancouver, Alberta, V5Z 4E6, Canada|London Regional Cancer Program, London, Ontario, N6A 4L6, Canada|Ottawa Regional Cancer Centre, Ottawa, Ontario, K1H 8L6, Canada|Princess Margaret Cancer Centre, Toronto, Ontario, M5G 2M9, Canada Less <<
NCT00658671 Advanced Cancer PHASE1 COMPLETED 2025-06-12 University of Colorado Hospita... More >>l, Aurora, Colorado, 80045, United States|Dana Farber/Harvard Cancer Center, Boston, Massachusetts, United States Less <<
NCT02234986 Advanced Adult Hepatocellular ... More >>Carcinoma|Advanced Fibrolamellar Carcinoma Less << PHASE2 COMPLETED 2018-06-30 CASI Site 03, San Francisco, C... More >>alifornia, 94158, United States|CASI Site 04, Aurora, Colorado, 80045, United States|CASI Site 02, Boston, Massachusetts, 01003, United States|Casi Site 01, New York, New York, 10065, United States|CASI Site 05, Dallas, Texas, 75231, United States Less <<
NCT01639248 Triple Negative Breast Cancer PHASE2 COMPLETED 2025-06-17 University of Colorado Cancer ... More >>Center, Aurora, Colorado, 80045, United States|Inidiana University Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Cancer Hospital of Chinese Academy of Medical Science, Beijing, 100021, China Less <<
NCT01719744 Advanced|Metastatic|Soft Tissu... More >>e Sarcoma Less << PHASE2 COMPLETED 2025-01-16 Princess Margaret Cancer Centr... More >>e, Toronto, Ontario, M5G 2M9, Canada Less <<
NCT00904787 Relapsed or Refractory Hematol... More >>ogical Malignancies Less << PHASE1 COMPLETED 2025-05-11 Princess Margaret Hospital, To... More >>ronto, Ontario, M5G 2M9, Canada Less <<
NCT00806065 Multiple Myeloma PHASE1 COMPLETED 2025-01-12 Indiana University Melvin and ... More >>Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States Less <<
NCT01104675 Ovarian Cancer|Fallopian Cance... More >>r|Peritoneal Cancer Less << PHASE2 COMPLETED 2025-12-12 University of Colorado Cancer ... More >>Center, Aurora, Colorado, 80045, United States|University of Chicago Medical Center, Chicago, Illinois, 60637, United States|Indiana University Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Dana Farber/Partners Cancer Care, Boston, Massachusetts, 02115, United States|Memorial Sloan-Kettering Cancer Center, New York, New York, United States|Princess Margaret Hospital, Toronto, Ontario, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.63mL

5.33mL

2.66mL

References

 

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