化合物简介
Oprozomib (INN, codenamed ONX 0912 and PR-047) is an orally active second-generation proteasome inhibitor developed by Onyx Pharmaceuticals, an Amgen subsidiary. It is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase 1b studies ongoing (as of February 16, 2016). Being an epoxyketone derivative, oprozomib is structurally related to carfilzomib and has the added benefit of being orally bioavailable. It selectively inhibits chymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7). Like carfilzomib, it is active against bortezomib-resistant multiple myeloma cells.
基本信息
中文名称
Oprozomib
英文名称
N-[(2S)-3-methoxy-1-[[(2S)-3-methoxy-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide
中文别名
英文别名
ONX-0912、QC-9273、Oprozomib、PR-047
CAS号
935888-69-0
分子式
C25H32N4O7S
分子量
532.609
精确质量
532.199
PSA
186.96
LOGP
2.6684
编号系统
UNII
MZ37792Y8J
合成路线
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