Onartuzumab (MetMAb) 是一种人源化亲和成熟的单价单克隆抗体,抑制受体酪氨酸激酶MET。Onartuzumab 可有效抑制 HGF 结合、受体磷酸化和信号转导。Onartuzumab 具有抗体样药代动力学和抗肿瘤活性。
生物活性 | Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against theMETreceptor. Onartuzumab potently inhibitsHGFbinding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity[1]. |
体外研究 (In Vitro) | Onartuzumab acts specifically by blocking HGF α-chain (but not β-chain) binding to MET[1]. Onartuzumab blocks HGF binding to human c-Met with an inhibitory concentration (IC)50 of 1.8 nM and inhibits the subsequent induction of c-Met auto-phosphorylation and cell proliferation in many cancer cell lines[2].
|
体内研究 (In Vivo) | Onartuzumab (30 mg/kg, IP, twice a week for 2 mouth) suppresses tumor growth[3].
Animal Model: | Human HGF-transgenic SCID mice implanted with BxPC3 tumor cells, nude (nu/nu) mice implanted with KP4 human pancreatic xenograft tumor cells[3] | Dosage: | 30 mg/kg | Administration: | IP, twice a week for 2 mouth | Result: | Suppressed tumor growth, but did not affect the mean in vivo human HGF levels. |
Animal Model: | U-87 MG tumor-bearing mice[3] | Dosage: | 30 mg/kg | Administration: | IP, once | Result: | Resulted in profound TGI (tumor growth inhibition) with 4/10 mice demonstrating a partial response (>50% reduction in tumor size) and 6/10 mice demonstrating a complete response (100% tumor regression). |
|
Clinical Trial | |
CAS 号 | |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |