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Delanzomib

CAS No. : 847499-27-8

MCE 国际站：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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