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ln Vitro |
In SK-N-FI cells, bobatumumab (0.02-80 nM; 0.5 or 4 h) inhibits both basal and IGF-I-induced phosphorylation of IGF-IR and IRS-1[2]. It also downregulates IGF-IR.
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ln Vivo |
Robatumumab (intravenous injection; 0.04 or 0.1 mg/mouse; twice weekly; 18 d) inhibits the SK-N-FI tumor growth in xenograft model[2]. Robatumumab (intravenous injection; 0.02-0.5 mg/mouse; twice weekly; 35 d) inhibits the osteosarcoma growth in xenograft model[2]. Robatumumab (intravenous injection; 0.1 or 0.5 mg/mouse; twice weekly; 14 d) inhibits the SJCRH30 and RD rhabdomyosarcoma cell growth in xenograft model[2]. ; 0.1 or 0.5 mg/mouse; twice weekly; 2 w) blocks effectively pediatric tumor cell proliferation in vivo[2]. Robatumumab (intravenous injection; 0.5 mg/mouse; once; day 11 post-inoculation) modulates the blood vessel formation via its antiangiogenesis effect[2].
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Cell Assay |
Western Blot Analysis[2]
Cell Types: SK-N-FI cells Tested Concentrations: 0.02-80 nM Incubation Duration: 0.5 or 4 hrs (hours) Experimental Results: Inhibited the IGF-I–stimulated phosphorylation of IGF-IR after treatment 0.5 h. Resulted in both inhibition of IGF- IR phosphorylation and receptor downregulation after treatment 4 h. Resulted in a dose-dependent inhibition of the IGF-I–stimulated IRS-1 phosphorylation. |
Animal Protocol |
Animal/Disease Models: Nude mice inoculated with SK-N-FI tumor cells[2]
Doses: 0.04 or 0.1 mg/mouse Route of Administration: intravenous (iv) injection; 0.04 or 0.1 mg/mouse; twice weekly; 18 days Experimental Results: Inhibited the SK-N-FI xenograft tumor by 96% in the 0.04 mg dose group and resulted in 11% tumor regression in the 0.1 mg dose group. Animal/Disease Models: Nude mice inoculated with SJSA-1 osteosarcoma[2] Doses: 0.02 , 0.1 or 0.5 mg/mouse Route of Administration: intravenous (iv) injection; 0.02, 0.1 or 0.5 mg/mouse; twice weekly; 35 days Experimental Results: Inhibited the tumor growth by 71%, 82%, and 88% at 0.02, 0.1, and 0.5 mg , respectively, at day 14 after treatment. Animal/Disease Models: Nude mice inoculated with SJCRH30 and RD rhabdomyosarcoma cells[2] Doses: 0.1 or 0.5 mg/mouse Route of Administration: intravenous (iv) injection; 0.1 or 0.5 mg/mouse; twice weekly; 14 days Experimental Results: Inhibited tumor growth by 39% and 58% at 0.1 and 0.5 mg dose, respectively, in the RD rhabdomyosarcoma model. Inhibited tumor growth by 37% and 53% at 0.1 and 1 mg dose, re |
References |
[1]. Anderson PM, et al. A phase II study of clinical activity of SCH 717454 (robatumumab) in patients with relapsed osteosarcoma and Ewing sarcoma. Pediatr Blood Cancer. 2016 Oct;63(10):1761-70.
[2]. Wang Y, et al. A fully human insulin-like growth factor-I receptor antibody SCH 717454 (Robatumumab) has antitumor activity as a single agent and in combination with cytotoxics in pediatric tumor xenografts. Mol Cancer Ther. 2010 Feb;9(2):410-8. |
CAS # |
934235-44-6
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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.