IC50: 0.2 nM (CSF-1R)[2]
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) [1][2].
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].
Cell Viability Assay[2]
| Cell Line: | CSF-1 and/or GM-CSF Macrophages |
| Concentration: | 0-10 μg/mL |
| Incubation Time: | 7 days |
| Result: | Resulted cell death of CSF-1-differentiated macrophages. |
Emactuzumab(RG 7155) (i.v.; 0.1??1??10??30 and 100 mg/kg; once) increases CSF-1 concentration in nonhuman primates' peripheral blood[2].
RG7155 (i.v.; 0, 30, and 100 mg/kg; once weekly; for 2 weeks) depletes CSF-1R+CD163+ macrophages in vivo[2].
| Animal Model: | cynomolgus monkeys Macaca fascicularis[2] |
| 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. |