Figitumumab CP-751871|cas:943453-46-1|西域试剂

Figitumumab CP-751871,96.89%

产品编号：Bellancom-P99197| CAS NO：943453-46-1

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-P99197		￥4000.00	杭州北京（现货）
Bellancom-P99197		￥10000.00	杭州北京（现货）

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Figitumumab CP-751871

产品介绍

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 an IC₅₀ of 1.8 nM.

体外研究

Figitumumab (CP-751871) (152 pM-10 μM; 3 days) inhibits cancer cell proliferation.
Figitumumab (1 μg/mL; 1 min or 24 h) induces the down-regulation of IGF-1R.
Figitumumab inhibits IGF1-induced autophosphorylation of IGF1R with an IC₅₀ of 0.42 nM, and indirectly inhibits AKT activation.
Figitumumab recognizes the IGF-1R/IR heterodimer complex.

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

Cell Proliferation Assay

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 IC₅₀ values ≦ 100 nM.

Western Blot Analysis

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.

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.
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.

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

Animal Model:	Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF-1R tumors
Dosage:	31 to 125 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Resulted in a serum C_max between 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-1 nu/nu), human Colo-205 tumor xenograft model
Dosage:	62.5 μg or 250 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Inhibited the tumor growth.

体内研究

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

Animal Model:	Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF-1R tumors
Dosage:	31 to 125 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Resulted in a serum C_max between 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-1 nu/nu), human Colo-205 tumor xenograft model
Dosage:	62.5 μg or 250 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Inhibited the tumor growth.

体内研究

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

Animal Model:	Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF-1R tumors
Dosage:	31 to 125 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Resulted in a serum C_max between 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-1 nu/nu), human Colo-205 tumor xenograft model
Dosage:	62.5 μg or 250 μg per mouse
Administration:	Intraperitoneal injection, once
Result:	Inhibited the tumor growth.