WebApr 14, 2024 · M1774, a potent, selective, orally administered ATR inhibitor with antitumor activity in preclinical models, was evaluated in Part A1 of an open-label, single-arm study (NCT04170153) for safety, tolerability, maximum tolerated dose, pharmacokinetics (PK) and pharmacodynamics (PD). WebJan 1, 2024 · Caffeine and wortmannin (a fungal metabolite) (Fig. 4) are among the earliest agents used in the pioneering preclinical studies to demonstrate the sensitisation potential of ATR inhibition (IC50 = 1.1 mM and 1.8 μM respectively) to IR and other genotoxic agents on cancer cells, although these agents were also observed to inhibit multiple PIKKs ( …
Abstract 6210: Combination of M1774 and niraparib can overcome ATR …
WebMay 31, 2024 · M1774 will be administered orally once daily over a defined period of time in Part A1 and Part B1 until disease progression, death, discontinuation, or end of … WebJun 3, 2024 · The company has advanced the development of its orally administered ataxia telangiectasia and Rad3-related (ATR) inhibitor M1774. Following completion of the monotherapy dose-escalation part of the DDRiver Solid Tumors 301 study, a monotherapy dose for M1774 has been confirmed for further evaluation in Phase Ib. Findings, which … mnsi webmail login email
EMD Serono Advances Development Programs in …
WebJun 4, 2024 · The company has advanced the development of its orally administered ataxia telangiectasia and Rad3-related (ATR) inhibitor M1774. Following completion of the monotherapy dose-escalation part of the DDRiver Solid Tumors 301 study, a monotherapy dose for M1774 has been confirmed for further evaluation in Phase Ib. Findings, which … WebHere, we report the ATR kinase inhibitor AZD6738 (Ceralasertib) and analogues thereof as bona fide inhibitors of TAF1. Crystallographic and small-angle X-ray scattering studies established that newly identified and previously reported inhibitors stabilize distinct structural states of the TAF1 tandem bromodomain through “open–closed ... WebJun 15, 2024 · M1774 is a potent inhibitor of ATR protein kinase with high selectivity towards other protein kinases. A broad range of antiproliferative activities (ranging from … mns international edition