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CEP-18770
- русский язык имя
- английское имяCEP-18770
- CAS №847499-27-8
- CBNumberCB42570998
- ФормулаC21H28BN3O5
- мольный вес413.28
- номер MDLMFCD18251439
- файл Mol847499-27-8.mol
химическое свойство
Температура плавления | 178-190°C (dec.) |
плотность | 1.207 |
температура хранения | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
растворимость | Acetonitrile (Slightly), Chloroform (Slightly), Methanol (Slightly) |
форма | Solid |
пка | 9.67±0.43(Predicted) |
цвет | White to Off-White |
Стабильность | Hygroscopic |
FDA UNII | 6IF28942WO |
Словарь наркотиков NCI | delanzomib |
CEP-18770 химические свойства, назначение, производство
Описание
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.Использование
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.CEP-18770 поставщик
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