Product Description: Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2-/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice[1].
Applications: Cancer-programmed cell death
Formula: C20H14D3ClF4N4O2
References: [1]Wang Y, et al., Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors. Bioorg Med Chem. 2024 Apr 1;103:117662.