Emactuzumab
Based on 1 Customer Validation
Emactuzumab(RG 7155) is a specific monoclonal antibody that inhibits colonystimulating factor 1 receptor (CSF1R) activation. Emactuzumab has high affinity for CSF-1R with Ki value of 0.2 nM to blocks CSF-1R dimerization. Emactuzumab can be used for the research of several diseases, such as diffuse-type tenosynovial giant cell tumour (dt-GCT) .
For research use only. We do not sell to patients.
- Purity: 97.60%
- CAS No.: 1448221-67-7
- Molecular Weight:144.41 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Human IgG1 kappa
Human
CSF1R/M-CSFR/CD115
Emactuzumab (RG 7155) binds to human and cynomolgus CSF-1R with high affinity (Kd=0.2 nM) to blocks CSF-1R dimerization[2].
RG7155 (0-10 μg/mL, 7 days) potently inhibited the viability of CSF-1-differentiated macrophages with an IC50 of 0.3 nM by inducing cell death[2].
RG7155 (30 μg/mL, 6 days) induces cell death of in vitro-differentiated human M2-like macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CSF-1 and/or GM-CSF Macrophages
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Concentration:0-10 μg/mL
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Incubation Time:7 days
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Result:Resulted cell death of CSF-1-differentiated macrophages.
RG7155 (i.v.; 0, 30, and 100 mg/kg; once weekly; for 2 weeks) depletes CSF-1R+CD163+ macrophages in vivo[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:cynomolgus monkeys Macaca fascicularis[2]
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Dosage:0.1, 1, 10, 30 and 100 mg/kg (male cynomolgus monkeys)
0, 30, and 100 mg/kg (male and female cynomolgus) -
Administration:i.v., once (male cynomolgus monkeys)
i.v., once weekly, for 2 weeks(male and female cynomolgus) -
Result:Increased CSF-1 concentration in serum.
Efficiently reduced CSF-1R and CD68+163+ macrophages in the liver (Kupffer cells) and colon of cynomologus monkeys.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
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Immobilized CSF1R Protein, Human (HEK293, HY-P72948) can bind Emactuzumab. The EC50 for this effect is 8.427 ng/mL. -
Flow cytometric analysis of 1.5X106 THP-1 cells with Emactuzumab (HY-P99245, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. 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, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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CAS No. 1448221-67-7
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Appearance Liquid
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Molecular Weight 144.41 kDa
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Color Colorless to light yellow
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SMILES
[Emactuzumab]
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Synonyms
RG 7155; RO 5509554
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (260 KB)
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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)
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Inhibitory Antibodies User Guide (603 KB)
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)