General Information of the Drug (ID: M6ADRUG0054)
Name
PLX4032
Synonyms
PLX4032; RG7204; RO5185426; Zelboraf (TN); Vemurafenib (BRAF inhibitor)
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Status Approved [1]
Structure
Formula
C23H18ClF2N3O3S
InChI
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
InChIKey
GPXBXXGIAQBQNI-UHFFFAOYSA-N
PubChem CID
42611257
TTD Drug ID
D0Y9EW
DrugBank ID
DB08881
Full List of m6A Targets Related to This Drug
Epidermal growth factor receptor (EGFR)
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary METTL3 increased the m6A modification of Epidermal growth factor receptor (EGFR) mRNA in A375R cells, which promoted its translation efficiency. Inhibiting METTL3 function to restore PLX4032 sensitivity in patients with melanoma.
Responsed Disease Melanoma ICD-11: 2C30
Target Regulator Methyltransferase-like 3 (METTL3) WRITER
Target Regulation Up regulation
Pathway Response EGFR tyrosine kinase inhibitor resistance hsa01521
Cell Process Cell apoptosis
In-vitro Model A375-R Amelanotic melanoma Homo sapiens CVCL_6234
References
Ref 1 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: 5893).
Ref 2 METTL3 induces PLX4032 resistance in melanoma by promoting m(6)A-dependent EGFR translation. Cancer Lett. 2021 Dec 1;522:44-56. doi: 10.1016/j.canlet.2021.09.015. Epub 2021 Sep 13.