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| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| ln Vitro |
Dalotuzumab (h7C10; 33 nM; 24 h) suppresses the growth of MCF7 estrogen-dependent breast cancer cells stimulated by IGF-1 and IGF-2, with IC50 values of 4.2 and 3.1 nM, respectively [1]. In IGF-1-induced MCF7 cells, dalotuzumab (33 nM; 24 h) causes cycle arrest and prevents IGF-IR and IRS-1 autophosphorylation [1]. MCF7 and A459 cells' NK cell-mediated lysis rates were raised by dalotuzumab by 26% and 25%, respectively [1]. In endometrial cancer cells, dalotuzumab (MK-0646; 10 µg/mL; 24, 48 h) eliminates the anti-apoptotic action of IGF1 [2].
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| ln Vivo |
Dalotuzumab (h7C10; intraperitoneal; 250 µg/mouse initially, then 125 µg/mouse twice weekly for 40 days) exhibits antitumor properties in tumor models xenografted with MCF-7 and A549 [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF7 cells (IGF-1 and IGF-2-induced) Tested Concentrations: 33 nM Incubation Duration: 24 h Experimental Results: demonstrated anti-proliferation activity to IGF-1- and IGF-2-induced MCF7, with IC50 values of 4.2 and 3.1 nM, respectively. Cell Cycle Analysis[1] Cell Types: MCF7 cells (IGF-1-induced ) Tested Concentrations: 33 nM Incubation Duration: 24 h Experimental Results: Prevented cell cycle progression from the G1 to S and G2/M phases. Apoptosis Analysis[2] Cell Types: ECC-1 and USPC-1 cells (IGF-1-induced) Tested Concentrations: 10 µg/mL Incubation Duration: 24, 48 h Experimental Results: Reversed the effect of IGF1 on caspase-3 cleavage (Caspase-3 is activated in apoptotic cells and cleaves several cellular proteins, including PARP). Western Blot Analysis[1] Cell Types: MCF7 cells (IGF-1-induced) Tested Concentrations: 33 nM Incubation Duration: 24 h Experimental Results: Led to a decrease of phosphorylation for both β-chain and IRS-1. |
| Animal Protocol |
Animal/Disease Models: Swiss Nude mice (MCF-7 and A549 xenograft tumor models)[1].
Doses: 125 and 250 (first time) µg/mice Route of Administration: intraperitoneal (ip)injection; 250 µg/mice for the first time, then 125 µg/mice twice weekly for 40 days Experimental Results: Led to average tumor volume at 6 weeks post-cell injection was diminished by 70% and 72% in the MCF-7 and A549 models, respectively. |
| 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.
[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. [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. |
| Molecular Weight |
146.4 (kDa)
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| CAS # |
1005389-60-5
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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