EPZ-5676_1380288-87-8_DataSheet_MedChemExpress

P d t D t Sh t Product Name:

EPZ-5676CAS No.:

1380288-87-8Cat. No.:

HY-15593

Product Data Sheet

MWt:

562.71Formula:

C30H42N8O3Purity :>98%

Solubility:

DMSO 100 mg/ml; Water <1 mg/ml

Mechanisms:

Biological Activity:

EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase with Ki of 80pM;demonstrating >37000fold selectivity against all other PMTs tested inhibits

Pathways:Cell Cycle/DNA Damage; Target:HMTase with Ki of 80 pM; demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits

H3K79 methylation in tumor.

IC50 Value: 80 pM (Ki value) [1]

Target: in vitro: The compound has a Ki value of 80 pM, and demonstrates 37,000-fold selectivity over all other methyltransferases tested. In cellular studies, EPZ-5676inhibited H3K79 methylation and MLL-fusion target gene expression and demonstrated potent cell killing that was selective for acute

leukemia lines bearing MLL translocations [1].in vivo: Continuous intravenous (IV) infusion of EPZ-5676 in a rat xenograft model of MLL-References:

[1]. Daigle SR, Olhava EJ, Therkelsen CA, Potent inhibition of DOT1L as treatment for MLL-fusion

leukemia. Blood. 2013 Jun 25. [Epub ahead of print]rearranged leukemia caused complete tumor regressions that were sustained well beyond the

compound infusion period with no significant weight loss or signs of toxicity [1].Clinical tri...

Caution: Not fully tested. For research purposes only

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