EPZ004777

CAS NO.：1338466-77-5
Empirical Formula: C28H41N7O4
Molecular Weight: 539.67
MDL number: MFCD25563264
SAFETY DATA SHEET (SDS)
Update Date: 2025-12-08 19:11:55

What is EPZ004777?

The Uses of EPZ004777

EPZ 004777 is potent small molecule inhibitor of protein lysine methyltransferase DOT1L.

Definition

ChEBI: 1-[3-[[(2R,3S,4R,5R)-5-(4-amino-7-pyrrolo[2,3-d]pyrimidinyl)-3,4-dihydroxy-2-oxolanyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea is a N-glycosyl compound.

Biological Activity

epz004777 is a specific small-molecule h3k79 methyltransferase dot1l inhibitor that potently inhibits dot1l in a radionuclide homogeneous assay with the half maximal inhibition concentration ic50 value of 400 pm and selectively kills a variety of mll-rearranged leukemia cells, including an mll-af4 leukemia cell line mv4-11 and an mll-af9 leukemia cell line molm13 [1 & 2].epz004777 has also been found to selectively inhibit the proliferation of mll-af10 and calm-af10 transformed cells in a dose dependent manner (ic50: 0.1 μm to 1 μm), in which the mrna expression levels of two hallmark leukemogenic genes (hoxa9 and meis1) are suppressed by epz004777 in a concentration dependent manner [2].

Storage

Store at -20°C

Properties of EPZ004777

Boiling point:	740.7±60.0 °C(Predicted)
Density	1.33±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	≥27 mg/mL in DMSO; insoluble in H2O; ≥94.6 mg/mL in EtOH with ultrasonic
form	solid
pka	12.51±0.70(Predicted)
color	White to off-white

Safety information for EPZ004777

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.