OPROZOMIB (ONX-0912)

Description: Oprozomib (formerly known as ONX 0912 and PR 047) is a novel, potent, and orally bioavailable small molecule inhibitor for chymotrypsin-like (CT)-L activity of 20S proteasome beta5/LMP7 with potential antitumor activity. It inhibits 20S proteasome beta5/LMP7 with IC50 of 36 nM/82 nM. Oprozomib exhibited high antitumor activity in vivo in multiple human tumor xenograft and mouse syngeneic models.

References: J Med Chem. 2009 May 14; 52(9):3028-38; Blood. 2010 Dec 2; 116(23):4906-15.

Chemical Name: N-((S)-3-methoxy-1-(((S)-3-methoxy-1-(((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)amino)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)-2-methylthiazole-5-carboxamide

InChi Key: SWZXEVABPLUDIO-WSZYKNRRSA-N

InChi Code: InChI=1S/C25H32N4O7S/c1-15-26-11-20(37-15)24(33)29-19(13-35-4)23(32)28-18(12-34-3)22(31)27-17(21(30)25(2)14-36-25)10-16-8-6-5-7-9-16/h5-9, 11, 17-19H, 10, 12-14H2, 1-4H3, (H, 27, 31)(H, 28, 32)(H, 29, 33)/t17-, 18-, 19-, 25+/m0/s1

SMILES Code: O=C(C1=CN=C(C)S1)N[CH](COC)C(N[CH](COC)C(N[CH](CC2=CC=CC=C2)C([C]3(C)OC3)=O)=O)=O