935888-69-0

• 常用中文名：Oprozomib (ONX 0912)
• 常用英文名：Oprozomib (ONX 0912)
• CAS号：935888-69-0
• 分子式：C₂₅H₃₂N₄O₇S
• 分子量：532.609
• 相关类别： 生物化工 抑制剂 蛋白酶体(Proteases) Proteasome 抑制剂
• 发布时间：2018-12-24 13:03:22
• 更新时间：2024-01-05 10:39:24
• Oprozomib (ONX 0912; PR047)是口服生物相容性的抑制剂,能抑制20S proteasome(20S蛋白酶体)β5/LMP7的CT-L活性,IC50为36 nM/82 nM。

名称

• 中文名: Oprozomib
• 英文名: 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
• 英文别名: ONX-0912; 4,5-Anhydro-1,2-dideoxy-4-methyl-2-({O-methyl-N-[(2-methyl-1,3-thiazol-5-yl)carbonyl]-L-seryl-O-methyl-L-seryl}amino)-1-phenyl-D-erythro-pent-3-ulose; QC-9273; PR-047; ONX 0912; D-erythro-3-Pentulose, 4,5-anhydro-1,2-dideoxy-4-C-methyl-2-[[O-methyl-N-[(2-methyl-5-thiazolyl)carbonyl]-L-seryl-O-methyl-L-seryl]amino]-1-phenyl-

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 849.9±65.0 °C at 760 mmHg
• 分子式: C₂₅H₃₂N₄O₇S
• 分子量: 532.609
• 闪点: 467.8±34.3 °C
• 精确质量: 532.199158
• PSA: 186.96000
• LogP: 2.79
• 外观性状: 粉末
• 蒸汽压: 0.0±3.2 mmHg at 25°C
• 折射率: 1.573
• 储存条件: -20℃

生物活性

• 描述: Oprozomib (ONX 0912; PR047)是口服生物相容性的抑制剂,能抑制20S proteasome(20S蛋白酶体)β5/LMP7的CT-L活性,IC50为36 nM/82 nM。
• 相关类别:
  信号通路 >> 自噬 >> 自噬
  信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体
  研究领域 >> 癌症
• 参考文献:

  [1]. Zhou HJ, et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem. 2009 May 14;52(9):3028-38.

  [2]. Chauhan D, et al. A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood, 2010, 116(23), 4906-4915.

  [3]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis. Nat Med, 2009, 15(7), 781-787.

合成路线

1148157-29-2 1010136-49-8 ~86% 935888-69-0

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 ;

40004-69-1 1148157-34-9 ~% 935888-69-0

文献：Zhou, Han-Jie; Aujay, Monette A.; Bennett, Mark K.; Dajee, Maya; Demo, Susan D.; Fang, Ying; Ho, Mark N.; Jiang, Jing; Kirk, Christopher J.; Laidig, Guy J.; Lewis, Evan R.; Lu, Yan; Muchamuel, Tony; Parlati, Francesco; Ring, Eileen; Shenk, Kevin D.; Shields, Jamie; Shwonek, Peter J.; Stanton, Timothy; Sun, Congcong M.; Sylvain, Catherine; Woo, Tina M.; Yang, Jinfu Journal of Medicinal Chemistry, 2009 , vol. 52, # 9 p. 3028 - 3038

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文献：US2014/113855 A1, ;

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文献：US2014/113855 A1, ;

1010136-50-1 ~% 935888-69-0

文献：US2014/113855 A1, ;

935888-09-8 ~% 935888-69-0

文献：US2014/113855 A1, ;

1148157-33-8 ~% 935888-69-0

文献：US2014/113855 A1, ;

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