| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| Other Sizes |
| Targets |
IC50: 1.8 nM (IGF1R)[1]
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|---|---|
| ln Vitro |
CP-751871, figitumumab (152 pM–10 μM; 3 days) inhibits the growth of cancer cells[1]. IGF-1R is down-regulated by figitumumab (1 μg/mL; 1 min or 24 h)[2]. With an IC50 of 0.42 nM, figitumumab prevents IGF1-induced autophosphorylation of IGF1R and obstructs AKT activation indirectly[2]. One can identify the IGF-1R/IR heterodimer complex with figitumumab [2].
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| ln Vivo |
Figitumumab (CP-751871) (31-125 μg/mouse; ip; once) induces the down-regulation of tumor associated IGF-1R in mice[2]. Figitumumab (62.5-500 μg/mouse; ip; once) inhibits the growth of sc xenografts derived from colon (Colo-205), breast (MCF7), and lung (H460) cancer cell lines in mice[2].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Breast, colon , lung small cell, and non-small cell cancer lines Tested Tested Concentrations: 152 pM-10 μM Incubation Duration: 3 days Experimental Results: 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[2] Cell Types: 3T3/IGF-1R cell Tested Tested Concentrations: 1 μg/mL Incubation Duration: 1 min or 24 h Experimental Results: Blocked IGF-I- or IGF-II-induced autophosphorylation of the IGF-1R. |
| Animal Protocol |
Animal/Disease Models: Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF -1R tumors[2]
Doses: 31 to 125 μg per mouse Route of Administration: intraperitoneal (ip) injection, once Experimental Results: Resulted in a serum Cmax between 12 and 24 hrs (hours). At 24 hrs (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/Disease Models: Female athymic mice (CD-1 nu/nu), human Colo-205 tumor xenograft model[2] Doses: 62.5 μg or 250 μg per mouse Route of Administration: intraperitoneal (ip) injection, once Experimental Results: Inhibited the tumor growth. |
| References |
[1]. Pavlicek A, et al. Molecular predictors of sensitivity to the insulin-like growth factor 1 receptor inhibitor Figitumumab (CP-751,871). Mol Cancer Ther. 2013 Dec;12(12):2929-39.
[2]. Cohen BD, et al. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871. Clin Cancer Res. 2005 Mar 1;11(5):2063-73. |
| CAS # |
943453-46-1
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|---|---|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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