CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 of 0.55 nM. It enhances the effects of DNA-damaging agents on tumor cells and exhibits synergistic anticancer activity with Gemcitabine.

Chk1:0.55 nM

CHK1-IN-9 (compound 11) demonstrates antiproliferative effects on tumor cells at concentrations of 11.11, 33.33, 100, and 300 nM over a 16-hour period, with an IC50 value of 202 nM specifically for MV-4-11 cells.

CHK1-IN-9 (compound 11) administered at 30 mg/kg daily for 21 consecutive days, either intravenously or orally, results in a tumor growth inhibition (TGI) of 20.6% when used alone on HT-29 xenograft mouse models. When combined with Gemcitabine, it demonstrates enhanced antitumor activity with a TGI of 42.8%.