Products
Petosemtamab Biosimilar Bispecific Antibody (EGFR × LGR5) for Research
Pre-Made Petosemtamab biosimilar, Bispecific mAb, Anti-EGFR;LGR5 Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2;FEX/GPR49/GPR67/GRP49/HG38 therapeutic antibody is a biosimilar expressed by mammalian cell line as a benchmark reference therapeutic antibody for biological drug disovery items including cell culture, assay development, animal model development, PK/PD model development (Pharmacokinetics & Pharmacodynamic) and mechanism of action (MOA) research.
Petosemtamab (also known as MCLA 158) is a bispecific, full length human IgG antibody being developed by Merus, for the treatment of solid tumours including.
Order Information
| Catalog No. | Package | Price(In USD) |
|---|---|---|
| GMP-Bios-ab-440-1mg | 1mg | |
| GMP-Bios-ab-440-10mg | 10mg | |
| GMP-Bios-ab-440-100mg | 100mg | |
| GMP-Bios-ab-440-xmg | ＞100mg |
Product Details
| Products Name (INN Index) | Pre-Made Petosemtamab biosimilar, Bispecific mAb, Anti-EGFR;LGR5 Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2;FEX/GPR49/GPR67/GRP49/HG38 therapeutic antibody |
| INN Name | Petosemtamab |
| Target | EGFR;LGR5 |
| Format | Bispecific mAb |
| Derivation | Bispecific antibody |
| Species Reactivity | Human |
| CH1 Isotype | IgG1 |
| VD LC | Kappa;Kappa |
| Highest_Clin_Trial (Jan '20) | Phase-I |
| Est. Status | Discontinued |
| 100% SI Structure | None;None |
| 99% SI Structure | None;None |
| 95-98% SI Structure | None;None |
| Year Proposed | 2019 |
| Year Recommended | 2020 |
| Companies | Merus |
| Conditions Approved | na |
| Conditions Active | na |
| Conditions Discontinued | na |
| Development Tech | na |
About target - EGFR
1. Protein Epidermal growth factor receptor
2. Gene EGFR
3. Organism Homo sapiens (Human)
Function
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:2790960, PubMed:10805725, PubMed:27153536).
Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF (PubMed:2790960, PubMed:7679104, PubMed:8144591, PubMed:9419975, PubMed:15611079, PubMed:12297049, PubMed:27153536, PubMed:20837704, PubMed:17909029).
Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules (PubMed:27153536).
May also activate the NF-kappa-B signaling cascade (PubMed:11116146).
Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling (PubMed:11602604).
Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin (PubMed:11483589).
Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration (PubMed:20462955).
Plays a role in enhancing learning and memory performance (By similarity).
Isoform 2 may act as an antagonist of EGF action.
(Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry. Mediates HCV entry by promoting the formation of the CD81-CLDN1 receptor complexes that are essential for HCV entry and by enhancing membrane fusion of cells expressing HCV envelope glycoproteins.
Catalytic activityi
ATP + L-tyrosyl-[protein] = ADP + H+ + O-phospho-L-tyrosyl-[protein]
EC:2.7.10.1
Source: Rhea.
Activity regulationi
Endocytosis and inhibition of the activated EGFR by phosphatases like PTPRJ and PTPRK constitute immediate regulatory mechanisms. Upon EGF-binding phosphorylates EPS15 that regulates EGFR endocytosis and activity. Moreover, inducible feedback inhibitors including LRIG1, SOCS4, SOCS5 and ERRFI1 constitute alternative regulatory mechanisms for the EGFR signaling. Up-regulated by NEU3-mediated desialylation of N-linked glycan at Asn-528.
