CAS 935888-69-0|Oprozomib (ONX 0912)

Introduction：Basic information about CAS 935888-69-0|Oprozomib (ONX 0912), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Oprozomib (ONX 0912) BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Oprozomib (ONX 0912)
CAS Number	935888-69-0	Molecular Weight	532.609
Density	1.3±0.1 g/cm3	Boiling Point	849.9±65.0 °C at 760 mmHg
Molecular Formula	C₂₅H₃₂N₄O₇S	Melting Point	/
MSDS	/	Flash Point	467.8±34.3 °C

Names

Name	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
Synonym	More Synonyms

Oprozomib (ONX 0912) BiologicalActivity

Description	Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1]Target: 20S proteasomeThe anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models.
Related Catalog	Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Metabolic Enzyme/Protease >>ProteasomeResearch Areas >>Cancer
References	[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.

Description

Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1]Target: 20S proteasomeThe anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models.

Related Catalog

Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Metabolic Enzyme/Protease >>ProteasomeResearch Areas >>Cancer

References

[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.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	849.9±65.0 °C at 760 mmHg
Molecular Formula	C₂₅H₃₂N₄O₇S
Molecular Weight	532.609
Flash Point	467.8±34.3 °C
Exact Mass	532.199158
PSA	186.96000
LogP	2.79
Vapour Pressure	0.0±3.2 mmHg at 25°C
Index of Refraction	1.573
InChIKey	SWZXEVABPLUDIO-WSZYKNRRSA-N
SMILES	COCC(NC(=O)c1cnc(C)s1)C(=O)NC(COC)C(=O)NC(Cc1ccccc1)C(=O)C1(C)CO1
Storage condition	-20℃

Synonyms

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-

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