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Oprozomib

Oprozomib

  • CAT Number: I005559
  • CAS Number: 935888-69-0
  • Molecular Formula: C₂₅H₃₂N₄O₇S
  • Molecular Weight: 532.61
  • Purity: ≥95%
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Oprozomib(CAT: I005559), also known as ONX 0912 or PR047, is an orally bioavailable inhibitor of the CT-L (chymotrypsin-like) activity of the 20S proteasome β5/LMP7 subunit. It exhibits potent anti-multiple myeloma (MM) activity by inducing apoptosis through the activation of caspase-8, caspase-9, caspase-3, and PARP. Oprozomib also inhibits the migration of MM cells and angiogenesis, contributing to its anti-cancer effects. In preclinical studies, Oprozomib has demonstrated favorable pharmacokinetics with a high absolute bioavailability in rodents and dogs. It is well tolerated and can achieve significant proteasome inhibition in various tissues, leading to antitumor responses in multiple tumor models.

Catalog Number I005559
CAS Number 935888-69-0
Molecular Formula

C₂₅H₃₂N₄O₇S

Purity 95%
Target Proteasome
Solubility DMSO: ≥ 50 mg/mL
Storage Store at -20°C
IC50 36 nM/82 nM(20S proteasome β5/LMP7)
InChI 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
InChIKey SWZXEVABPLUDIO-WSZYKNRRSA-N
SMILES CC1=NC=C(S1)C(=O)NC(COC)C(=O)NC(COC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C
Reference

<br />
1:In Vitro Metabolism of Oprozomib, an Oral Proteasome Inhibitor: Role of Epoxide Hydrolases and Cytochrome P450s. Wang Z, Fang Y, Teague J, Wong H, Morisseau C, Hammock BD, Rock DA, Wang Z.Drug Metab Dispos. 2017 Apr 20. pii: dmd.117.075226. doi: 10.1124/dmd.117.075226. [Epub ahead of print] PMID: 28428366 <br />
2:Anti-angiogenic and anti-multiple myeloma effects of oprozomib (OPZ) alone and in combination with pomalidomide (Pom) and/or dexamethasone (Dex). Sanchez E, Li M, Wang CS, Tang G, Gillespie A, Chen H, Berenson JR.Leuk Res. 2017 Mar 6;57:45-54. doi: 10.1016/j.leukres.2017.03.002. [Epub ahead of print] Review. PMID: 28288323 <br />
3:Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma. Vandewynckel YP, Coucke C, Laukens D, Devisscher L, Paridaens A, Bogaerts E, Vandierendonck A, Raevens S, Verhelst X, Van Steenkiste C, Libbrecht L, Geerts A, Van Vlierberghe H.Oncotarget. 2016 Jun 7;7(23):34988-5000. doi: 10.18632/oncotarget.9222. PMID: 27167000 Free PMC Article<br />
4:A first-in-human dose-escalation study of the oral proteasome inhibitor oprozomib in patients with advanced solid tumors. Infante JR, Mendelson DS, Burris HA 3rd, Bendell JC, Tolcher AW, Gordon MS, Gillenwater HH, Arastu-Kapur S, Wong HL, Papadopoulos KP.Invest New Drugs. 2016 Apr;34(2):216-24. doi: 10.1007/s10637-016-0327-x. Epub 2016 Feb 29. PMID: 26924128 <br />
5:Validation of the 2nd Generation Proteasome Inhibitor Oprozomib for Local Therapy of Pulmonary Fibrosis. Semren N, Habel-Ungewitter NC, Fernandez IE, K&#246;nigshoff M, Eickelberg O, St&#246;ger T, Meiners S.PLoS One. 2015 Sep 4;10(9):e0136188. doi: 10.1371/journal.pone.0136188. eCollection 2015. PMID: 26340365 Free PMC Article<br />
6:Carfilzomib and oprozomib synergize with histone deacetylase inhibitors in head and neck squamous cell carcinoma models of acquired resistance to proteasome inhibitors. Zang Y, Kirk CJ, Johnson DE.Cancer Biol Ther. 2014 Sep;15(9):1142-52. doi: 10.4161/cbt.29452. Epub 2014 Jun 10. PMID: 24915039 Free PMC Article<br />
7:The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4. Zang Y, Thomas SM, Chan ET, Kirk CJ, Freilino ML, DeLancey HM, Grandis JR, Li C, Johnson DE.Autophagy. 2012 Dec;8(12):1873-4. doi: 10.4161/auto.22185. Epub 2012 Sep 20. PMID: 22995770 Free PMC Article<br />
8:The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects. Hurchla MA, Garcia-Gomez A, Hornick MC, Ocio EM, Li A, Blanco JF, Collins L, Kirk CJ, Piwnica-Worms D, Vij R, Tomasson MH, Pandiella A, San Miguel JF, Garayoa M, Weilbaecher KN.Leukemia. 2013 Feb;27(2):430-40. doi: 10.1038/leu.2012.183. Epub 2012 Jul 5. PMID: 22763387 Free PMC Article

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