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编 号:F741215
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CAS No: 1448221-67-7
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生物活性:
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) .
体内研究:
Emactuzumab(RG 7155) (i.v.; 0.1、1、10、30 and 100 mg/kg; once) increases CSF-1 concentration in nonhuman primates’ peripheral blood.RG7155 (i.v.; 0, 30, and 100 mg/kg; once weekly; for 2 weeks) depletes CSF-1R+CD163+ macrophages in vivo.Animal Model:cynomolgus monkeys Macaca fascicularis
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.
体外研究:
Emactuzumab (RG 7155) binds to human and cynomolgus CSF-1R with high affinity (Kd = 0.2 nM) to blocks CSF-1R dimerization.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.RG7155 (30 μg/mL, 6 days) induces cell death of in vitro-differentiated human M2-like macrophages.