Size | Price | |
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1mg | ||
5mg | ||
Other Sizes |
Targets |
IC50: 0.2 nM (CSF-1R)[2]
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ln Vitro |
Emactuzumab (RG 7155) inhibits CSF-1R dimerization by binding to human and cynomolgus CSF-1R with a high affinity (Kd = 0.2 nM)[2]. With an IC50 of 0.3 nM, RG7155 (0-10 μg/mL, 7 days) significantly reduced the viability of CSF-1-differentiated macrophages by causing cell death[2]. RG7155 (30 μg/mL, 6 days) causes human M2-like macrophages that have been developed in vitro to die[2].
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ln Vivo |
Emactuzumab (RG 7155) (iv; 0.1, 1, 10, 30 and 100 mg/kg; once) raises the level of CSF-1 in the peripheral blood of nonhuman primates[2]. CSF-1R+CD163+ macrophages are depleted in vivo by RG7155 (iv; 0, 30, and 100 mg/ kg; once weekly; for 2 weeks)[2].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: CSF-1 and/or GM-CSF Macrophages Tested Concentrations: 0-10 μg/mL Incubation Duration: 7 days Experimental Results: Resulted cell death of CSF-1-differentiated macrophages. |
Animal Protocol |
Animal/Disease Models: cynomolgus monkeys Macaca fascicularis[2]
Doses: 0.1, 1, 10, 30 and 100 mg/kg (male cynomolgus monkeys ) 0, 30, and 100 mg/kg (male and female cynomolgus) Route of Administration: iv, once (male cynomolgus monkeys) iv, once weekly, for 2 weeks (male and female cynomolgus) Experimental Results: Increased CSF-1 concentration in serum. Efficiently decreased CSF-1R and CD68+163+ macrophages in the liver (Kupffer cells) and colon of cynomologus monkeys. |
References |
[1]. Philippe A Cassier, et al. CSF1R inhibition with emactuzumab in locally advanced diffuse-type tenosynovial giant cell tumours of the soft tissue: a dose-escalation and dose-expansion phase 1 study. Lancet Oncol. 2015 Aug;16(8):949-56.
[2]. Carola H Ries, et al. Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy. Cancer Cell. 2014 Jun 16;25(6):846-59. |
CAS # |
1448221-67-7
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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 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.) |
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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.