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

ENMD-2076 

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

ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

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  

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Other Forms of ENMD-2076:

    ENMD-2076 purchased from MCE. Usage Cited in: Int J Gynecol Cancer. 2017 Oct;27(8):1666-1674.

    Enhanced cytotoxicity in OCCC cells treated with ENMD-2076 plus Cisplatin. Western blot analysis showing that phospho-Aurora-A protein levels are decreased at 0.5-12 hours after treatment with ENMD-2076.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

    IC50 & Target

    IC50: 1.86 nM (Aurora A), 14 nM (Flt3), 58.2 nM (KDR/VEGFR2), 15.9 nM (Flt4/VEGFR3), 92.7 nM (FGFR1), 70.8 nM (FGFR2), 20.2 nM (Src), 56.4 nM (PDGFRα)[1]

    In Vitro

    ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM[1].

    In Vivo

    ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6633 mL 13.3166 mL 26.6333 mL
    5 mM 0.5327 mL 2.6633 mL 5.3267 mL
    10 mM 0.2663 mL 1.3317 mL 2.6633 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Recombinant Aurora A and B kinase enzymes 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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    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 9 doses of compound, spanning 0.3 nM to 125 mM, for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    ENMD-2076 is formulated in 0.075% carboxymethylcellulose, 0.085% Tween 80 in water[1].

    Mouse: Cell lines are injected subcutaneously or into the mammary fat pad (MDA-MB-231 only) of 5- to 6-week-old CB.17 SCID or NCr nude mice. Tumors are allowed to grow for 10 to 50 days before drug treatment. All treatments are with ENMD-2076 in water or ENMD-2076 free base in CMC-Tween vehicle (0.075% carboxymethylcellulose, 0.085% Tween 80 in water), administered orally. Percent tumor growth inhibition is calculated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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

    DMSO: ≥ 31 mg/mL

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

    Purity: 98.77%

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