General Information of the Drug (ID: M6APDG01263)
Name
MGCD516
Synonyms
Sitravatinib
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Status
Phase 2/3
Structure
Formula
C33H29F2N5O4S
InChI
1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42)
InChIKey
WLAVZAAODLTUSW-UHFFFAOYSA-N
PubChem CID
25212148
TTD Drug ID
D05BLN
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Proto-oncogene c-Met (MET)
Methyltransferase-like 3 (METTL3)
In total 2 mechanisms lead to this potential drug response
Response Summary Proto-oncogene c-Met (MET) is a therapeutic target for MGCD516. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of MGCD516 through regulating the expression of Proto-oncogene c-Met (MET). [1], [2]
Proto-oncogene c-Met (MET) is a therapeutic target for MGCD516. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of MGCD516 through regulating the expression of Proto-oncogene c-Met (MET). [1], [3]
References
Ref 1 RNA m(6) A methylation regulates uveal melanoma cell proliferation, migration, and invasion by targeting c-Met. J Cell Physiol. 2020 Oct;235(10):7107-7119. doi: 10.1002/jcp.29608. Epub 2020 Feb 4.
Ref 2 Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209. doi: 10.1158/2159-8290.CD-20-0116. Epub 2020 May 15.
Ref 3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7948).