Pinometostat

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

Product Specifications

CAS Number

[1380288-87-8]

Product Name Alternative

EPZ-5676

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/EPZ-5676.html

Purity

99.99

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 100 mg/mL (ultrasonic)

Smiles

NC1=NC=NC2=C1N=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN([C@@H]4C[C@H](CCC5=NC6=C(C=CC(C(C)(C)C)=C6)N5)C4)C(C)C)O3

Molecular Formula

C30H42N8O3

Molecular Weight

562.71

Precautions

H302, H315, H319, H335

References & Citations

[1]Daigle SR, et al. Potent inhibition of DOT1L as treatment for MLL-fusion leukemia. Blood. 2013 Jun 25. [Epub ahead of print]|[2]Klaus CR, et al. DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells. J Pharmacol Exp Ther. 2014 Sep;350 (3) :646-56.