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Dalotuzumab

Cat. No. M24531
Dalotuzumab Structure
Synonym:

MK-0646; h7C10

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Biological Activity

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 drugs such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo.

Chemical Information
CAS Number 1005389-60-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xiao Qu, et al. Oncotarget. Update of IGF-1 receptor inhibitor (ganitumab, dalotuzumab, cixutumumab, teprotumumab and figitumumab) effects on cancer therapy

[2] Francesco Sclafani, et al. Int J Cancer. Dalotuzumab in chemorefractory KRAS exon 2 mutant colorectal cancer: Results from a randomised phase II/III trial

[3] Didier Frappaz, et al. Eur J Cancer. Phase 1 study of dalotuzumab monotherapy and ridaforolimus-dalotuzumab combination therapy in paediatric patients with advanced solid tumours

[4] Teresa Moran, et al. Exp Hematol Oncol. Activity of dalotuzumab, a selective anti-IGF1R antibody, in combination with erlotinib in unselected patients with Non-small-cell lung cancer: a phase I/II randomized trial

[5] Mario Scartozzi, et al. Curr Opin Mol Ther. Dalotuzumab, a recombinant humanized mAb targeted against IGFR1 for the treatment of cancer

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Keywords: Dalotuzumab, MK-0646; h7C10 supplier, IGF-1R, inhibitors, activators


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