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Delanzomib
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Delanzomib
CAS No. : 847499-27-8
MCE 站:Delanzomib
产品活性:Delanzomib (CEP-18770) 是一种强效的具有口服活性的蛋白酶体的胰凝乳蛋白酶样活性 (chymotrypsin-like activity of the proteasome) 抑制剂,IC50 为 3.8 nM。Delanzomib 抑制 NF-κB 活性,诱导癌细胞凋亡 (apoptotic),并具有很强的抗血管生成和抗癌活性。
研究领域:Metabolic Enzyme/Protease | NF-κB | Apoptosis
作用靶点:Proteasome | NF-κB | Apoptosis
In Vitro: Delanzomib (CEP-18770; 20 nM; 12-24 hours) treatment results in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines, RPMI-8226, and U266.
Delanzomib (CEP-18770; 5-40 nM; 4-24 hours) treatment induces an accumulation of ubiquitinated proteins over 4 to 8 hours.
Delanzomib (CEP-18770) inhibits endothelial cell survival, vasculogenesis, and osteoclastogenesis in vitro; and displays a favorable cytotoxicity profile toward normal cells.
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.
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