Figitumumab (CP-751871) 是一种有效的全人抗胰岛素样生长因子 1 受体 (IGF1R) 单克隆抗体。Figitumumab 可阻止 IGF1 与 IGF1R 结合，IC50为 1.8 nM。
| 生物活性 | Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with anIC50of 1.8 nM[1]. |
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体外研究
(In Vitro) | Figitumumab (CP-751871) (152 pM-10 μM; 3 days) inhibits cancer cell proliferation[1].
Figitumumab (1 μg/mL; 1 min or 24 h) induces the down-regulation of IGF-1R[2].
Figitumumab inhibits IGF1-induced autophosphorylation of IGF1R with an IC50of 0.42 nM, and indirectly inhibits AKT activation[2].
Figitumumab recognizes the IGF-1R/IR heterodimer complex[2].
Cell Proliferation Assay[1] | Cell Line: | Breast, colon, lung small cell, and non–small cell cancer lines | | Concentration: | 152 pM-10 μM | | Incubation Time: | 3 days | | Result: | 15 cell lines (NCIH441, NCIH526, SW403, CACO2, SW48, NCIH524, SKCO1, SNUC1, LS1034, COLO205, MDAMB361, NCIH508, LS513, MCF7, NCIH378) were highly sensitive to the drug at IC50values ≦ 100 nM. |
Western Blot Analysis[2] | Cell Line: | 3T3/IGF-1R cell | | Concentration: | 1 μg/mL | | Incubation Time: | 1 min or 24 h | | Result: | Blocked IGF-I- or IGF-II-induced autophosphorylation of the IGF-1R. |
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体内研究
(In Vivo) | Figitumumab (CP-751871) (31-125 μg/mouse; i.p.; once) induces the down-regulation of tumor associated IGF-1R in mice[2].
Figitumumab (62.5-500 μg/mouse; i.p.; once) inhibits the growth of s.c. xenografts derived from colon (Colo-205), breast (MCF7), and lung (H460) cancer cell lines in mice[2].
| Animal Model: | Female athymic mice (CD-1nu/nu) bearing NIH3T3/IGF-1R tumors[2] | | Dosage: | 31 to 125 μg per mouse | | Administration: | Intraperitoneal injection, once | | Result: | Resulted in a serum Cmaxbetween 12 and 24 hours. At 24 hours, there was a dose-dependent reduction of IGF-1R protein in tumors, with 50% reduction observed at a serum concentration of 15 μg/mL. Resulted in a down-regulation of IGF-1R from the tumor. The half-life in an athymic mouse was determined to be 4 to 6 days by longer-term studies. |
| Animal Model: | Female athymic mice (CD-1nu/nu), human Colo-205 tumor xenograft model[2] | | Dosage: | 62.5 μg or 250 μg per mouse | | Administration: | Intraperitoneal injection, once | | Result: | Inhibited the tumor growth. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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