Dalotuzumab  (Synonyms: MK-0646; h7C10)

Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo^[1][2][3].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Human

IGF1R/CD221

Dalotuzumab (h7C10; 33 nM; 24 h) inhibits IGF-1- and IGF-2-induced proliferation of MCF7 estrogen-dependent breast cancer cells with IC₅₀ values of 4.2 and 3.1 nM, respectively^[1].
Dalotuzumab (33 nM; 24 h) induces cycle arrest and inhibits autophosphorylation of the IGF-IR and IRS-1, in MCF7 cells (IGF-1-induced)^[1].
Dalotuzumab increases NK cell-mediated lysis of MCF7 and A459 cells by 26 and 25%, respectively^[1].
Dalotuzumab (MK-0646; 10 µg/mL; 24, 48 h) abrogates the anti-apoptotic effect of IGF1 in endometrial cancer cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dalotuzumab (h7C10; i.p.; 250 µg/mice for the first time, then 125 µg/mice twice weekly for 40 days) shows anti-tumor effects on MCF-7 and A549 xenograft tumor models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

3480  [NCBI]

P08069

ELISA, FACS, Functional assay

Unconjugated

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

146.78 kDa

1005389-60-5

Liquid

Colorless to light yellow

[Dalotuzumab]

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

• 
  Immobilized Human IGF1R Protein (ECD, His Tag) can bind Dalotuzumab. The EC₅₀ for this effect is 0.98 ng/mL.
• 
  Flow cytometric analysis of 1X10⁶ MCF-7 cells with Dalotuzumab (HY-P99284, 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.

• [1]. Goetsch L, et al. A recombinant humanized anti-insulin-like growth factor receptor type I antibody (h7C10) enhances the antitumor activity of vinorelbine and anti-epidermal growth factor receptor therapy against human cancer xenografts. Int J Cancer. 2005 Jan 10;113(2):316-28.  [Content Brief]

  [2]. Bitelman C, et al. IGF1R-directed targeted therapy enhances the cytotoxic effect of chemotherapy in endometrial cancer. Cancer Lett. 2013 Jul 10;335(1):153-9.  [Content Brief]

  [3]. Scartozzi M, et al. Dalotuzumab, a recombinant humanized mAb targeted against IGFR1 for the treatment of cancer. Curr Opin Mol Ther. 2010 Jun;12(3):361-71.  [Content Brief]