Art. -Nr.: HY-10987A

ENMD-2076

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

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.

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Reinheit: 99.99%
CAS. Nr.: 934353-76-1
Formel: C₂₁H₂₅N₇
Molecular Weight:375.47

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ENMD-2076 Chemical Structure

CAS. Nr.: 934353-76-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Aurora A

14 nM (IC₅₀)

KDR

58.2 nM (IC₅₀)

Flt-4

15.9 nM (IC₅₀)

FGFR1

92.7 nM (IC₅₀)

FGFR2

70.8 nM (IC₅₀)

PDGFRα

56.4 nM (IC₅₀)

Flt3

1.86 nM (IC₅₀)

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.65 μM Compound: ENMD-2076	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 37207533]
HeLa	IC₅₀	9.02 μM Compound: ENMD-2076	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 37207533]
L02	IC₅₀	42.62 μM Compound: ENMD-2076	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 37207533]
MDA-MB-231	IC₅₀	0.48 μM Compound: ENMD-2076	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32058239]
MDA-MB-231	IC₅₀	5.21 μM Compound: ENMD-2076	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 37207533]
PC-3	IC₅₀	0.67 μM Compound: ENMD-2076	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32058239]
SJSA-1	IC₅₀	56.67 μM Compound: ENMD-2076	Antiproliferative activity against human SJSA-1 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human SJSA-1 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 37207533]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 934353-76-1
Appearance Solid
Molecular Weight 375.47
Formel C₂₁H₂₅N₇
Color White to light yellow
SMILES

CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
NPJ Precis Oncol

Targeting high-risk MYC-overexpressed osteosarcoma with an Aurora kinase inhibitor:--results from a pilot umbrella trial. [Abstract]

2025 Dec 10. PMID: 41372533
Int J Gynecol Cancer

Inhibition of Aurora Kinase A Synergistically Enhances Cytotoxicity in Ovarian Clear Cell Carcinoma Cell Lines Induced by Cisplatin: A Potential Treatment Strategy. [Abstract]

2017 Oct;27(8):1666-1674. PMID: 28786875

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

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.
Am J Pathol

Antitumor Activity of a Novel Fibroblast Growth Factor Receptor Inhibitor for Intrahepatic Cholangiocarcinoma. [Abstract]

2019 Oct;189(10):2090-2101. PMID: 31351075

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 31 mg/mL (82.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.66 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37. [Content Brief]

[2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6633 mL	13.3166 mL	26.6333 mL	66.5832 mL
	5 mM	0.5327 mL	2.6633 mL	5.3267 mL	13.3166 mL
	10 mM	0.2663 mL	1.3317 mL	2.6633 mL	6.6583 mL
	15 mM	0.1776 mL	0.8878 mL	1.7756 mL	4.4389 mL
	20 mM	0.1332 mL	0.6658 mL	1.3317 mL	3.3292 mL
	25 mM	0.1065 mL	0.5327 mL	1.0653 mL	2.6633 mL
	30 mM	0.0888 mL	0.4439 mL	0.8878 mL	2.2194 mL
	40 mM	0.0666 mL	0.3329 mL	0.6658 mL	1.6646 mL
	50 mM	0.0533 mL	0.2663 mL	0.5327 mL	1.3317 mL
	60 mM	0.0444 mL	0.2219 mL	0.4439 mL	1.1097 mL
	80 mM	0.0333 mL	0.1665 mL	0.3329 mL	0.8323 mL

Keywords

ENMD-2076

4 Cited Publications

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ENMD-2076

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ENMD-2076

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle PDGFR Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ENMD-2076 Related Classifications

HY-10987A Related Classifications