Figitumumab
Based on 1 Customer Validation
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.
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- Pureté : 99.10%
- CAS No.: 943453-46-1
- Masse moléculaire:144.5 kDa
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
Isotype
Human IgG2 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
IGF1R/CD221
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 IC50 of 0.42 nM, and indirectly inhibits AKT activation[2].
Figitumumab recognizes the IGF-1R/IR heterodimer complex[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Breast, colon, lung small cell, and non–small cell cancer lines
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Concentration:152 pM-10 μM
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Incubation Time:3 days
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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.
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Cell Line:3T3/IGF-1R cell
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Concentration:1 μg/mL
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Incubation Time:1 min or 24 h
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Result:Blocked IGF-I- or IGF-II-induced autophosphorylation of the IGF-1R.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF-1R tumors[2]
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Dosage:31 to 125 μg per mouse
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Administration:Intraperitoneal injection, once
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Result:Resulted in a serum Cmax 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.
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Animal Model:Female athymic mice (CD-1 nu/nu), human Colo-205 tumor xenograft model[2]
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Dosage:62.5 μg or 250 μg per mouse
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Administration:Intraperitoneal injection, once
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Result:Inhibited the tumor growth.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG2 kappa
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized IGF-I R Protein, Human (HEK293, His, HY-P72606) can bind Figitumumab. The EC50 for this effect is 17.54 ng/mL. -
Flow cytometric analysis of 1X106 MCF-7 cells with Figitumumab (HY-P99197, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG2 kappa (HY-P99002, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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CAS No. 943453-46-1
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Appearance Liquid
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Masse moléculaire 144.5 kDa
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Color Colorless to light yellow
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SMILES
[Figitumumab]
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Synonyms
CP-751871
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Livraison
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureté et documentation
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Fiche technique (262 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Figitumumab Related Classifications
HY-P99197 Related Classifications
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