7-(3-(pyrrolidin-1-yl)propoxy)-6-methoxy-2-(5-methylfuran-2-yl)-N-((1-methylpiperidin-4-yl)methyl)quinolin-4-amine Chemical Properties

Boiling point:

641.8±55.0 °C(Predicted)

Density 

1.143±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

pka

10.09±0.20(Predicted)

7-(3-(pyrrolidin-1-yl)propoxy)-6-methoxy-2-(5-methylfuran-2-yl)-N-((1-methylpiperidin-4-yl)methyl)quinolin-4-amine Usage And Synthesis

Description

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1].

The Kd of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC50s of 92 nM and 1000 nM, respectively[1].

References

[1]. San José-Enériz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424.