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| | CEP-18770 Basic information |
| Product Name: | CEP-18770 | | Synonyms: | CEP-18770;[(1R)-1-[[(2S,3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid;CIP 18770;CT 47098;Delanzomib;NPH 007098;CEP-18770 (DelanzoMib);DelanzoMib, Free Base, >99% | | CAS: | 847499-27-8 | | MF: | C21H28BN3O5 | | MW: | 413.28 | | EINECS: | | | Product Categories: | Inhibitor;Inhibitors | | Mol File: | 847499-27-8.mol |  |
| | CEP-18770 Chemical Properties |
| Melting point | 178-190°C (dec.) | | density | 1.207 | | storage temp. | Hygroscopic, -20°C Freezer, Under Inert Atmosphere | | solubility | Acetonitrile (Slightly), Chloroform (Slightly), Methanol (Slightly) | | form | Solid | | pka | 9.67±0.43(Predicted) | | color | White to Off-White | | Stability: | Hygroscopic |
| | CEP-18770 Usage And Synthesis |
| Description | Delanzomib is an orally bioavailable inhibitor of chymotrypsin-like proteasome activity (IC50 = 3.8 nM in isolated human erythrocytes) that only marginally inhibits tryptic and peptidyl glutamyl proteasome activity. Delanzomib pre-treatment (20 nM) in vitro inhibits IκBα degradation, NF-κB activation, and the expression of NF-κB-regulated genes, including IκBα, XIAP, TNF-α, IL-1β, ICAM-1, and VEGF. Delanzomib induces apoptosis in multiple myeloma cell lines and inhibits proliferation in a panel of human hematologic and solid tumor cell lines (IC50s = 5.6-34.2 nM). It reduces tumor weight in an RPMI 8226 human multiple myeloma mouse xenograft model when administered intravenously at doses ranging from 1.5-4 mg/kg twice daily and leads to complete tumor regression at a chronic oral dose of 13 mg/kg. Delanzomib reduces the serum level of circulating cytokines, prevents renal tissue damage, and increases lifespan in a mouse model of fatal lupus nephritis. | | Uses | Delanzomib is an orally active proteasome inhibitor. Delanzomib has been shown to down-modulate NF-κB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis. | | Definition | ChEBI: Delanzomib is a C-terminal boronic acid peptide inhibitor which induces apoptosis in multiple myeloma, hematological and solid tumor cell lines. It has a role as a proteasome inhibitor, an apoptosis inducer and an antineoplastic agent. It is a threonine derivative, a phenylpyridine, a C-terminal boronic acid peptide and a secondary alcohol. It is functionally related to a L-threonine. | | target | proteasome |
| | CEP-18770 Preparation Products And Raw materials |
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