Bioactivity | 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]. |
CAS | 2923508-77-2 |
Formula | C20H14D3ClF4N4O2 |
Molar Mass | 459.84 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Wang Y, et al., Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors. Bioorg Med Chem. 2024 Apr 1;103:117662. |