Web31 de jan. de 2011 · ONX0912 (formerly PR-047) is a novel orally available analogue of the proteasome inhibitor carfilzomib. Carfilzomib, in common with bortezomib, is administered intravenously, however, proteasome inhibitor therapy requires twice weekly dosing and therefore an orally available inhibitor would be advantageous. WebIxazomib Citrate (MLN-9708)23Sponsor: Millennium PharmaceuticalsMW/cLogD: 517.1/–CAS#: 1202402-80-8Start/End Date: Jun, 2012–Jun, 2014Indication: Relapsed and/or refractory multiple myelomaRoute of Admin: oral, 4mg on days 1, 8, and 15MOA: Proteasome inhibitorClinicalTrials. From: Annual Reports in Medicinal Chemistry, 2013.
APExBIO - Oprozomib (ONX-0912) Proteasome inhibitor CAS
Web20 de mai. de 2010 · ONX0912 exerts a different inhibitory profile on proteasome activities compared with bortezomib. 16 Previous reports indicate that bortezomib targets mainly the CT-L activity and to a lesser degree the C-L activity, 17 whereas ONX0912 affects mainly the CT-L, 16 but the effect of ONX0912 and bortezomib in inhibiting the … Web16 de nov. de 2012 · Michael R. Savona, Jesus G. Berdeja, Susan J Lee, Hansen Wong, Ju RueyJiuan Lee, Heidi H. Gillenwater, David S. Siegel; A Phase 1b Dose-Escalation … dwight marney
Selective inhibition of chymotrypsin-like activity of the ...
WebOprozomib (ONX-0912) (PR-047) ist ein oral bioverfÜgbarer und selektiver Peptid-Epoxyketon-Proteasom-Inhibitor mit IC50-Werten von 36 und 82 nM fÜr das Proteasom (⋲5) bzw. das Immunproteasom (LMP7). Oprozomib … Web2 de dez. de 2010 · The synthetic and naturally occurring inhibitors of the UPS pathway include peptide aldehydes, peptide boronates, nonpeptide inhibitors, peptide vinyl … Web20 de mai. de 2012 · e13077 Background: Oprozomib (ONX0912), a structural analog of carfilzomib, is an orally bioavailable proteasome inhibitor that irreversibly binds to its target and is being evaluated in hematologic malignancies and solid tumors (ST). In a dose-escalation study of once-daily (qd) ONX0912, the maximum tolerated dose (MTD) was … crystaljellyfish