W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research[1].
IC 50
NSD2: 17 nM (IC50)
References
[1] Wei J, et al. Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2. J Med Chem. 2024 Sep 4. DOI:10.1021/acs.jmedchem.4c00639
