1. Cell Cycle/DNA Damage
    Epigenetics
    Protein Tyrosine Kinase/RTK
  2. Aurora Kinase
    FLT3
    VEGFR

ENMD-2076 

Cat. No.: HY-10987A Purity: 98.77%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
ENMD-2076 Chemical Structure

ENMD-2076 Chemical Structure

CAS No. : 934353-76-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $150 In-stock
50 mg $450 In-stock
100 mg $650 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of ENMD-2076:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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. IC50 value: 14 nM (Aurora A); 1.86 nM (Flt3); 58.2 nM (VEGFR2) [1] Target: Flt3; Aurora A in vitro: 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 [1]. 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 [2]. 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 [1]. 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 [2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01914510 University Health Network, Toronto Ovarian Clear Cell Carcinoma September 2013 Phase 2
NCT01719744 University Health Network, Toronto Advanced|Metastatic|Soft Tissue Sarcoma January 2013 Phase 2
NCT01639248 CASI Pharmaceuticals, Inc.|University of Colorado, Denver|Indiana University Melvin and Bren Simon Cancer Center Triple Negative Breast Cancer July 2012 Phase 2
NCT02234986 CASI Pharmaceuticals, Inc. Advanced Adult Hepatocellular Carcinoma|Advanced Fibrolamellar Carcinoma October 2015 Phase 2
NCT00904787 CASI Pharmaceuticals, Inc. Relapsed or Refractory Hematological Malignancies April 2009 Phase 1
NCT00806065 CASI Pharmaceuticals, Inc. Multiple Myeloma December 2008 Phase 1
NCT00658671 CASI Pharmaceuticals, Inc. Advanced Cancer April 2008 Phase 1
NCT01104675 CASI Pharmaceuticals, Inc. Ovarian Cancer|Fallopian Cancer|Peritoneal Cancer April 2010 Phase 2
View MoreCollapse
References
Molecular Weight

375.47

Formula

C₂₁H₂₅N₇

CAS No.

934353-76-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.77%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ENMD-2076
Cat. No.:
HY-10987A
Quantity: