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  • Oprozomib

    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

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

CAS:935888-69-0
中文别名
英文别名:ONX-0912;QC-9273;Oprozomib;PR-047;
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

物化性质

安全信息

生产方法及用途

合成路线

  • 参考文献

    Jumaa, Mouhannad; Muchamuel, Tony; Bejugam, Naveen; Wong, Hansen; Kirk, Christopher J.; Vishram Manek, Rahul; Sharma, Sanjeev Patent: US2014/113855 A1, 2014 ; Location in patent: Paragraph 0279; 0305; 0306; 0307; 0308 ;

上游原料

下游产品

图谱

1H NMR : Predict


13C NMR : Predict


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