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。

Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC 50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.

Solid

IC50: 3.8 nM (Chymotrypsin-like activity of the proteasome)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Piva R, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood. 2008 Mar 1;111(5):2765-75.

In Vitro: DMSO : 100 mg/mL (241.97 mM; Need ultrasonic)配制储备液