Intetumumab
Based on 1 Customer Validation
Intetumumab (CNTO 95) is a human monoclonal antibody targeting αv integrin, with a Kd value of 1-24 nM. Through high-affinity binding to αv integrin, Intetumumab inhibits its interaction with extracellular matrix proteins (such as vitronectin and fibronectin), thereby blocking the downstream focal adhesion kinase signaling pathway. This further inhibits the adhesion, migration and invasion of tumor cells as well as the proliferation of vascular endothelial cells, promotes cell apoptosis, and exerts anti-tumor and anti-angiogenic effects. Intetumumab can be used in research related to head and neck cancer, non-small cell lung cancer and uterine serous papillary carcinoma.
For research use only. We do not sell to patients.
- Purity: 99.24%
- CAS No.: 725735-28-4
- Molecular Weight:145.14 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Human IgG1 kappa
Human
Integrin aV/ITGAV/CD51
Intetumumab binds human αv integrin with a Kd of 1-24 nmol/L and rat αv integrin with a Kd of 220 nmol/L[1].
Intetumumab (0.15-5 μg/mL; 15 min pre-incubation with cells, 20 min incubation on coated plates) significantly inhibits adhesion of primary uterine serous papillary carcinoma cell lines to vitronectin, with 30% to 65% inhibition (P < 0.003)[2].
Intetumumab (1.25-20 μg/mL; 48 h incubation during migration assay) significantly inhibits migration of primary uterine serous papillary carcinoma cell lines through an 8.0-μm pore membrane, with 17% to 27% inhibition in USPC-ARK-2 cells (P < 0.03)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary uterine serous papillary carcinoma cell lines (USPC-ARK-2, USPC-ARK-4, USPC-ARK-6)
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Concentration:1.25, 5, 20 μg/mL
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Incubation Time:48 h (incubation during migration assay)
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Result:Inhibited migration of USPC-ARK-2 cells by 17% to 27% relative to control cells without antibody.
Showed a statistically significant effect at all tested concentrations.
Induced similar significant inhibition in USPC-ARK-4 and USPC-ARK-6 cell lines.
Intetumumab (10 mg/kg; intraperitoneal injection; once weekly for 60 days) significantly reduces the lung metastasis rate of intravenously injected A549 cells, with the number of affected rats and the average number of metastatic lesions per lung decreased by 56% and 77%, respectively[1].
Monotherapy with Intetumumab (10 mg/kg; intraperitoneal injection; once weekly for 60 days) reduces spontaneous lung metastasis of subcutaneously implanted A549 xenografts by 67% and enhances the anti-metastatic efficacy of radiotherapy[1].
Intetumumab (10 mg/kg; intraperitoneal injection; single administration) does not significantly enhance the radiosensitivity of intestinal crypt stem cells in nude mice[1].
Intetumumab enhances the efficacy of radiotherapy in a nude mouse xenograft model of human small cell lung cancer, delays tumor growth and reduces metastasis, without increasing the radiosensitivity of intestinal crypt stem cells[2].
Intetumumab is well tolerated, showing no toxicity, histopathological changes, or adverse effects on physiological angiogenesis in cynomolgus monkeys following long-term administration[2].
Intetumumab exerts anti-tumor and anti-angiogenic activities in nude mice bearing human melanoma xenografts[2].
Intetumumab inhibits spontaneous metastasis of human breast cancer xenografts in nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude rats (male, 5-6 weeks old, 150-200 g, injected i.v. with A549 cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once weekly for 60 days
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Result:Reduced the proportion of rats with lung metastases from 9/10 in controls to 4/9.
Reduced the average number of metastatic lesions per lung from 56 in controls to 13.
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Animal Model:nude rats (male, 5-6 weeks old, 150-200 g, inoculated s.c. with A549 cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once weekly for 60 days
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Result:Reduced the average number of spontaneous metastatic lung lesions per lung from 18 in controls to 6.
Reduced the proportion of rats with lung metastases from 6/6 in controls to 4/6.
When combined with fractionated radiation, reduced the average number of metastatic lesions per lung from 18 in controls to 4, and reduced the proportion of rats with lung metastases from 6/6 in controls to 5/6.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
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Flow cytometric analysis of 1X106 MCF-7 cells with Intetumumab (HY-P99296, 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 IgG1 kappa (HY-P99001, 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. 725735-28-4
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Appearance Liquid
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Molecular Weight 145.14 kDa
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Color Colorless to light yellow
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SMILES
[Intetumumab]
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Synonyms
CNTO 95; Anti-Human CD51 Recombinant Antibody
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (264 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[1]. Ning S, et al. Anti-alphav integrin monoclonal antibody intetumumab enhances the efficacy of radiation therapy and reduces metastasis of human cancer xenografts in nude rats. Cancer Res. 2010;70(19):7591-7599. [Content Brief]
[2]. Bellone M, et al. Expression of αV-integrins in uterine serous papillary carcinomas; implications for targeted therapy with intetumumab (CNTO 95), a fully human antagonist anti-αV-integrin antibody. Int J Gynecol Cancer. 2011;21(6):1084-1090. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Intetumumab
- 725735-28-4
- CNTO 95
- Anti-Human CD51 Recombinant Antibody
- CNTO95
- CNTO-95
- Integrin
- Apoptosis
- radiosensitizing effects
- head and neck cancer
- human αv integrin
- xenograft tumors
- rat αv integrin
- antimetastatic effects
- non-small cell lung cancer
- antitumor effects
- αv integrin
- antiangiogenic effects
- Inhibitor
- inhibitor
- inhibit