Home Tools

EPZ004777

Catalog No. T3081 CAS 1338466-77-5

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

EPZ004777, CAS 1338466-77-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 247.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 558.00
1 mL * 10 mM (in DMSO)	In stock	$ 91.00

Bulk Inquiry

Select Batch

Purity: 99.32%

Purity: 98.99%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
Targets&IC50	DOT1L:0.4 nM
Kinase Assay	Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values.
Cell Research	For assessment of cell proliferation and viability in human cell lines, exponentially growing cells are plated, in triplicate, in 96-well plates in a ?nal volume of 150 ml. Cells are incubated in the presence of 3 μM (proliferation curve), or increasing concentrations (IC50 determination) of EPZ004777 up to 50 μM. Viable cell number is determined every 3–4 days for up to 18 days using the Guava Viacount assay and analyzed on a Guava EasyCyte Plus instrument according to the manufacturer’s protocol. On days of cell counts, growth media and EPZ004777 are replaced and cells split back to a density of 5×104 cells/well. Total cell number is expressed as split-adjusted viable cells per well. For each cell line, IC50 values are determined from concentration-dependence curves at each time point using Graphpad Prism software. Experiments to determine IC50 values continues until IC50 values stabilized (day 18 for THP-1 cells, day 14 for all other cell lines). For assessment of the effect of EPZ004777 treatment on transformed murine hematopoietic progenitors, cells from two independent transductions for each virus are plated in 24-well plates at a density of 0.5–1×105 cell/well in 1 ml media in 24-well plates and exposed to increasing concentrations of EPZ004777 up to 30 mM. Cells are counted and replated at equal cell numbers in fresh media with fresh compound every 3–4 days. For MTT assays, cells from serial replatings are harvested on day 10 and plated, in triplicate at 2×104 cells/well in 100 ml media with the appropriate concentration of EPZ004777. Cells are incubated for 2.5 days, the exposed to 10 ml MTT reagent for 3 hr, and lysed over night in 100 ml MTT- solubilization buffer (both from Cell Proliferation Kit I [MTT]). (Only for Reference)

Molecular Weight	539.67
Formula	C28H41N7O4
CAS No.	1338466-77-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 54 mg/mL (100 mM)

DMSO: 54 mg/mL (100 mM)

References and Literature

1. Daigle SR, et al. Cancer Cell. 2011, 20(1), 53-65. 2. Chen L, et al. Leukemia. 2013, 27(4), 813-822. 3. Deshpande AJ, et al. Blood. 2013, 121(13), 2533-2541. 4. Zhou Z, Chen H, Xie R, et al. Epigenetically modulated FOXM 1 suppresses dendritic cell maturation in pancreatic cancer and colon cancer[J]. Molecular oncology. 2019 Apr;13(4):873-893.

Citations

1. Zhou Z, Chen H, Xie R, et al. Epigenetically modulated FOXM 1 suppresses dendritic cell maturation in pancreatic cancer and colon cancer. Molecular Oncology. 2019, 13(4): 873-893

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Histone Modification Compound Library Nucleotide Compound Library Bioactive Compound Library Covalent Inhibitor Library Anti-Aging Compound Library Chromatin Modification Compound Library Reprogramming Compound Library Epigenetics Compound Library

Related Products

Related compounds with same targets

Bortezomib JTE-013 A09-003 Taurodeoxycholic acid sodium hydrate Dinaciclib WYE-132 Pyroxamide EI1

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EPZ004777 1338466-77-5 Apoptosis Chromatin/Epigenetic Histone Methyltransferase inhibit EPZ 004777 EPZ-004777 Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.