Chemical Properties
| form | Liquid |
| color | Colorless to light yellow |
Emibetuzumab Chemical Properties,Usage,Production
Description
Emibetuzumab is a bivalent antibody that blocks HGF- and MET-receptor interaction, leading to MET internalization and degradation.Uses
Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer[1].Clinical Use
A phase I study determined a tolerable dose for emibetuzumab to be 700–2000 mg as a monotherapy and in combination with erlotinib in NSCLC patients. It is currently being investigated in phase II in combination with erlotinib.in vivo
Emibetuzumab (LY2875358) (10 mg/kg; i.v.; once a week for 5 weeks) inhibits in vivo growth of glioblastoma U87MG xenograft tumors in mice[1].
Emibetuzumab (10 or 20 mg/kg; i.v.; single) downregulates levels of MET and pMET in the tumors of mice[1].
Emibetuzumab (10 mg/kg; i.v.; once a week for 3, 5 or 6 weeks) exhibits antitumor effects on MET-amplified xenograft mouse tumor models[1].
| Animal Model: | Athymic nude mice (U87MG tumor xenograft model)[1]. |
| Dosage: | 10 mg/kg |
| Administration: | Intravenous injection, once a week for 5 weeks. |
| Result: | Demonstrated a significant inhibition of tumor growth. |
| Animal Model: | Athymic nude mice (MKN45 xenograft tumor model)[1]. |
| Dosage: | 10 or 20 mg/kg |
| Administration: | Intravenous injection, single. |
| Result: | Reduced MET and pMET in the tumors by approximately 50% at both the 10 and 20 mg/kg doses by 72 hours post dose, and the reductions persisted to 14 days. |
| Animal Model: | Athymic nude mice (MET-amplified xenograft mouse tumor models)[1]. |
| Dosage: | 10 mg/kg |
| Administration: | Intravenous injection, once a week for 3, 5 or 6 weeks. |
| Result: | Resulted in a marked reduction in tumor growth in the MKN45/SNU-5/EBC-1 gastric xenograft tumors. |
References
[1] Liu L, et al. LY2875358, a neutralizing and internalizing anti-MET bivalent antibody, inhibits HGF-dependent and HGF-independent MET activation and tumor growth. Clin Cancer Res. 2014 Dec 1;20(23):6059-70. DOI:10.1158/1078-0432.CCR-14-0543Emibetuzumab Suppliers
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