Intetumumab  (Synonyms: CNTO 95; Anti-Human CD51 Recombinant Antibody)

Intetumumab (CNTO 95) is a human monoclonal antibody targeting αv integrin, with a K_d 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^[1][2].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Human

Integrin aV/ITGAV/CD51

Intetumumab binds human αv integrin with a K_d of 1-24 nmol/L and rat αv integrin with a K_d 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.

Monotherapy with Intetumumab (10 mg/kg; i.p.; once weekly for 60 days) induces moderate tumor growth inhibition, with overall response rates of 33% and 17% in FaDu and A549 xenografts, respectively. This agent also significantly enhances the efficacy of fractionated radiotherapy, increasing the overall response rates to 89% and 67% in the two models, respectively. Meanwhile, it normalizes tumor vasculature, alleviates hypoxia, increases apoptosis, and causes no additional toxicity^[1].
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.

3685  [NCBI] & 3688  [NCBI]

P06756

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

145.14 kDa

725735-28-4

Liquid

Colorless to light yellow

[Intetumumab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG1 kappa

• 
  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).

• [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.

  [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]