CSRM617

CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2), which acts as a master regulator of androgen receptor networks in metastatic castration-resistant prostate cancer (mCRPC) and a driver of phenotypic plasticity in small cell lung cancer (SCLC). The compound binds directly to the OC2-HOX domain with a Kd of 7.43 μM, leading to the suppression of metastasis and induction of apoptosis via the activation of Caspase-3 and PARP. In SCLC, OC2 inhibition by CSRM617 represses the neuroendocrine regulator ASCL1 and modulates c-MYC and Notch signaling pathways. Developed by Cedars-Sinai Medical Center, CSRM617 has demonstrated preclinical efficacy in prostate, gastric, and pituitary cancer models and is being explored as a potential therapeutic for various neoplasms and urogenital diseases.

Other names

CAS 1353749-74-2CAS1353749-74-2CAS-1353749-74-2CAS 787504-88-5CAS787504-88-5CAS-787504-88-5