For research use only. Not for therapeutic Use.
Oprozomib(Cat No.: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 |
| Synonyms | 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 |
| 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) |
| IUPAC 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 |
| 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)N[C@@H](COC)C(=O)N[C@@H](COC)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)[C@]3(CO3)C |
| Reference | <br /> |
