Telisotuzumab

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NCI: A monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Anti-c-Met monoclonal antibody ABT-700 binds to c-Met, thereby preventing c-Met binding to its ligand, HGF and the subsequent activation of the HGF/c-Met signaling pathway. This may cause cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.

Inn NameTelisotuzumab
Lab CodesABT-700
Chemical NameImmunoglobulin G1-kappa, anti-[Homo sapiens MET (met proto-oncogene, hepatocyte growth factor (HGF) receptor, HGFR, scatter factor (SF) receptor, HGF/SF receptor,receptor tyrosine-protein kinase c-met, papillary renal cell carcinoma 2, RCC P2)], humanized monoclonal antibody; gamma1 heavy chain (1-445) [humanized VH (Homo sapiens IGHV1-2*02 (92.90%) -(IGHD)- IGHJ4*01) [8.8.11] (1-118) -Homo sapiens IGHG1*03, G1m3 (CH1 (119-216), hinge K7>del, T8>C (223), T10>del (217-229), CH2 (230- 339), CH3 (340-444), CHS K>del (445)) (119-445)], (221- 218')-disulfide with kappa light chain (1’-218’) [humanized V-KAPPA (Homo sapiens IGKV4-1*01 (85.10%) - IGKJ4*01) [10.3.9] (1'-111') -Homo sapiens IGKC*01, Km3 (112'-218')]; dimer (223-223":225-225":228:228")-trisdisulfide
SequenceHeavy chain
QVQLVQSGAE VKKPGASVKV SCKASGYIFT AYTMHWVRQA PGQGLEWMGW 50
IKPNNGLANY AQKFQGRVTM TRDTSISTAY MELSRLRSDD TAVYYCARSE 100
ITTEFDYWGQ GTLVTVSSAS TKGPSVFPLA PSSKSTSGGT AALGCLVKDY 150
FPEPVTVSWN SGALTSGVHT FPAVLQSSGL YSLSSVVTVP SSSLGTQTYI 200
CNVNHKPSNT KVDKRVEPKS CDCHCPPCPA PELLGGPSVF LFPPKPKDTL 250
MISRTPEVTC VVVDVSHEDP EVKFNWYVDG VEVHNAKTKP REEQYNSTYR 300
VVSVLTVLHQ DWLNGKEYKC KVSNKALPAP IEKTISKAKG QPREPQVYTL 350
PPSREEMTKN QVSLTCLVKG FYPSDIAVEW ESNGQPENNY KTTPPVLDSD 400
GSFFLYSKLT VDKSRWQQGN VFSCSVMHEA LHNHYTQKSL SLSPG 445

Light chain
DIVMTQSPDS LAVSLGERAT INCKSSESVD SYANSFLHWY QQKPGQPPKL 50
LIYRASTRES GVPDRFSGSG SGTDFTLTIS SLQAEDVAVY YCQQSKEDPL 100
TFGGGTKVEI KRTVAAPSVF IFPPSDEQLK SGTASVVCLL NNFYPREAKV 150
QWKVDNALQS GNSQESVTEQ DSKDSTYSLS STLTLSKADY EKHKVYACEV 200
THQGLSSPVT KSFNRGEC 218

Disulfide bridges location
Intra-H (C23-C104) 22-96 145-201 260-320 366-424
22''-96'' 145''-201'' 260''-320'' 366''-424''
Intra-L (C23-C104) 23'-92' 138'-198'
23'''-92''' 138'''-198'''
Inter-H-L (h 5-CL 126) 221-218' 221''-218'''
Inter-H-H (h 11, h 14) 225-225'' 228-228'' (h 8>C) 223-223''

N-glycosylation sites
H CH2 N84.4:
296, 296''
Fucosylated complex bi-antennary CHO-type glycans
Chemical StructureTelisotuzumab.png
Cas Registry Number1781223-80-0
New Molecular EntityYes
OriginatorPierre Fabre
DeveloperAbbVie
Mechanism Of Actionc-Met receptor tyrosine kinase (c-MET) (MET) (HGFR) (c-Met proto-oncogene) inhibitor
Who Atc CodesL01 (Antineoplastic Agents)
Ephmra CodesL1 (Antineoplastics)
IndicationAdvanced Solid Tumors

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