Dalotuzumab
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 97.43%
- CAS No.: 1005389-60-5
- Molecular Weight:146.78 kDa
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Dalotuzumab
More
Biological Activity
Human IgG1 kappa
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.
-
Cell Line:MCF7 cells (IGF-1 and IGF-2-induced)
-
Concentration:33 nM
-
Incubation Time:24 h
-
Result:Showed anti-proliferation activity to IGF-1- and IGF-2-induced MCF7, with IC50 values of 4.2 and 3.1 nM, respectively.
-
Cell Line:MCF7 cells (IGF-1-induced)
-
Concentration:33 nM
-
Incubation Time:24 h
-
Result:Prevented cell cycle progression from the G1 to S and G2/M phases.
-
Cell Line:ECC-1 and USPC-1 cells (IGF-1-induced)
-
Concentration:10 µg/mL
-
Incubation Time:24, 48 h
-
Result:Reversed the effect of IGF1 on caspase-3 cleavage (Caspase-3 is activated in apoptotic cells and cleaves several cellular proteins, including PARP).
-
Cell Line:MCF7 cells (IGF-1-induced)
-
Concentration:33 nM
-
Incubation Time:24 h
-
Result:Led to a decrease of phosphorylation for both β-chain and IRS-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Swiss Nude mice (MCF-7 and A549 xenograft tumor models)[1].
-
Dosage:125 and 250 (first time) µg/mice
-
Administration:Intraperitoneal injection; 250 µg/mice for the first time, then 125 µg/mice twice weekly for 40 days
-
Result:Led to average tumor volume at 6 weeks post-cell injection was reduced by 70% and 72% in the MCF-7 and A549 models, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
-
Human IgG1 kappa
ELISA, FACS, Functional assay
-
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.
Chemical Information
-
CAS No. 1005389-60-5
-
Appearance Liquid
-
Molecular Weight 146.78 kDa
-
Color Colorless to light yellow
-
SMILES
[Dalotuzumab]
-
Synonyms
MK-0646; h7C10
-
Shipping
Shipping with dry ice.
-
Formulation
Please refer to the lot-specific COA for specific buffer information.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Mol Ther Oncol
Employing splice-switching oligonucleotides and AAVrh74.U7 snRNA to target insulin receptor splicing and cancer hallmarks in osteosarcoma. [Abstract]2024 Nov 23;32(4):200908. PMID: 39720325
Purity & Documentation
-
Data Sheet (265 KB)
-
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)
-
Inhibitory Antibodies User Guide (603 KB)
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)