EPZ004777

SKU: orb1226514

Description

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

Key Properties

• CAS Number: 1338466-77-5
• MW: 539.67
• Purity: >98% (HPLC)
• Formula: C₂₈H₄₁N₇O₄
• SMILES: O=C(NC1=CC=C(C(C)(C)C)C=C1)NCCCN(C[C@H]2O[C@@H](N3C=CC4=C(N)N=CN=C43)[C@H](O)[C@@H]2O)C(C)C
• Target: HMTase
• Solubility: Ethanol: 100 mg/mL (185.29 mM); DMSO: 100 mg/mL (185.29 mM)

Bioactivity

• In Vivo:
  EPZ004777 is well tolerated and no overt toxicity is observed. Complete blood count analysis after 14 days of continuous exposure to EPZ004777 revealed a statistically significant increase in the total white blood cell count, which resulted from an increase in neutrophils, monocytes, and lymphocytes. EPZ004777 (50, 100, or 150 mg/mL) administration is well tolerated, and no significant weight loss is observed.
• In Vitro:
  EPZ004777 demonstrates potent, concentration-dependent inhibition of DOT1 L enzyme activity with an IC50 of 400±100 pM. EPZ004777 displays remarkable selectivity for inhibition of DOT1 L over other HMTs(PRMT5, 521±137 nM; others, >50 μM). The effect of extended EPZ004777 treatment is remarkably specific for the MLL-rearranged cell lines. The number of viable MV4-11 and MOLM-13 cells is dramatically reduced by EPZ004777, whereas the growth of Jurkat cells is unaffected. A small population of MV4-11 cells remain viable in the presence of EPZ004777, but their number remain constant when growth curves are tracked over longer periods indicating that they have ceased to divide. The proliferation of MLL-AF9-transformed cells is strongly inhibited by EPZ004777 at concentrations of 3 μM or greater. EPZ004777 selectively inhibits proliferation of MLL-AF10 and CALM-AF10 transformed murine bone marrow cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EPZ004777 | EPZ 004777

Quick Database Links

Gene Symbol

HMTase