PKMYT1-IN-13

PKMYT1-IN-13 is a potent, orally active, and highly selective PKMYT1 inhibitor. It exhibits an IC50 value of less than 10.0 nM for PKMYT1 in ADP-Glo assays and 19.9 nM in NanoBRET cell assays, demonstrating significant selectivity over WEE1. This compound shows selective antiproliferative activity in CCNE1-amplified cells with minimal impact on wild-type cells. Furthermore, PKMYT1-IN-13 demonstrates notable antitumor activity in HCC1569 mouse xenograft models and is applicable for studying CCNE1-amplified cancers such as gastric, ovarian, and breast cancers.