CEP-18770
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
- 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.
in vivo
Delanzomib (CEP-18770; 7.8-13 mg/kg; oral administration; twice a week; for 4 weeks) treatment results in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues, complete tumor regression of multiple myeloma (MM) xenografts and improves overall median survival in a systemic model of human MM[1].
| Animal Model: | SCID mice injected with RPMI 8226 cells[1] |
| Dosage: | 7.8 mg/kg, 10 mg/kg, 13 mg/kg |
| Administration: | Oral administration; twice a week; for 4 weeks |
| Result: | Resulted in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues. |
target
proteasome
CEP-18770Supplier
- Tel
- sales@boylechem.com
- Tel
- 18210857532
- jkinfo@jkchemical.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 021-50135380
- shchemsky@sina.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
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