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Fig. 1 · Structure
Cat. No.
A12983
CAS No.
1338466-77-5
Formula
C28H41N7O4
Mol. Weight
539.67

Documents & Downloads

EPZ004777

Cat. No. A12983 CAS 1338466-77-5

DOT1L inhibitor

EPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes.

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Biological Activity

Target & Activity

Target Activity Value
DOT1L (Cell-free assay) 0.4 nM

Cellular Effect

Cell Line Activity Value Description Reference
697 IC50 > 10 μM Cytotoxicity against human 697 cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]
HL-60 IC50 > 10 μM Cytotoxicity against human HL60 cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]
Jurkat IC50 > 10 μM Cytotoxicity against human Jurkat cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]
Kasumi 1 IC50 > 10 μM Cytotoxicity against human Kasumi-1 cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]
MOLM-13 IC50 700 nM Inhibition of DOT1L in human MOLM13 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis 10.1039/C1MD00199J
MV4-11 IC50 700 nM Inhibition of DOT1L in human MV4-11 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis 10.1039/C1MD00199J
REH IC50 > 10 μM Cytotoxicity against human REH cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]
U-937 IC50 > 10 μM Cytotoxicity against human U937 cells assessed as cell viability measured every 3 to 4 days up to 18 days by Guava Viacount assay [PMID: 25406853]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1338466-77-5
Applications DOT1L inhibitor
Formula C28H41N7O4
Molecular Weight 539.67
SMILES
CC(C)N(CCCNC(=O)NC1=CC=C(C=C1)C(C)(C)C)C[C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C3N=CN=C4N)O)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 95 mg/mL (176.03 mM)
Water Insoluble
Ethanol 95 mg/mL (176.03 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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