m6A-centered Drug Response Information

General Information of the Drug (ID: M6ADRUG0100)
Name
Erlotinib
Synonyms
Erlotinib; 183321-74-6; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine; Erlotinib free base; 4-[(3-Ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline; OSI-774; UNII-J4T82NDH7E; 4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine; 183321-74-6 (free base); NSC 718781; CHEMBL553; J4T82NDH7E; [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE; CP358774; CHEBI:114785; MFCD02089651; NCGC00164574-01; [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine; DSSTox_CID_26454; DSSTox_RID_81628; DSSTox_GSID_46454; CP-358,774; Erlotinib(Tarceva); OSI-744; CAS-183321-74-6; NSC718781; RG-1415; Erlotinib [INN:BAN]; SR-05000001460; erlotinibum; Erotinib; R-1415; HSDB 8082; OSI 744; nchembio866-comp3; Erlotinib, Free Base; Kinome_3317; n-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine monohydrochloride; R 1415; SCHEMBL8413; BDBM5446; cid_176870; GTPL4920; DTXSID8046454; QCR-100; HMS2089F05; HMS3244M19; HMS3244M20; HMS3244N19; HMS3295A19; HMS3713C22; HMS3745M05; ZINC1546066; Tox21_112202; 3615AH; AC-399; NSC800097; s7786; STK623143; AKOS000282911; Tox21_112202_1; CCG-220420; CS-0620; DB00530; MCULE-7764565391; NSC-800097; Ro-508231; SB16916; NCGC00164574-03; NCGC00164574-05; NCGC00164574-06; NCGC00164574-14; NCGC00164574-25; AS-35132; BCB03_000783; BE164419; HY-50896; P443; SY028059; AM20090621; FT-0651539; R1415; CP-35877401; K00241; AB01273955-01; AB01273955-02; AB01273955-03; 321E746; Q418369; SR-05000001460-1; SR-05000001460-2; SR-05000001460-3; SR-05000001460-6; BRD-K70401845-003-04-7; n-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy) quinazolin-4-amine; 1429636-49-6
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Status Approved [1]
Structure
Formula
C22H23N3O4
InChI
InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
InChIKey
AAKJLRGGTJKAMG-UHFFFAOYSA-N
PubChem CID
176870
TTD Drug ID
D07POC
DrugBank ID
DB00530
Full List of m6A Targets Related to This Drug
LINC00902 (TUSC7)
 Target Info 
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary In lung adenocarcinoma, The miR-146a/Notch signaling was sustained highly activated in a m6A dependent manner, and the m6A regulator of YTHDF2 suppressed LINC00902 (TUSC7), both of which contributed to the resistant features. Functionally, the sponge type of TUSC7 regulation of miR-146a inhibited Notch signaling functions, and affected the cancer progression and stem cells' renewal in Erlotinib resistant PC9 cells (PC9ER) and Erlotinib resistant HCC827 cells (HCC827ER) cells.
Responsed Disease Lung adenocarcinoma ICD-11: 2C25.0
 Disease Info 
Target Regulator YTH domain-containing family protein 2 (YTHDF2) READER
 Regulator Info 
Target Regulation Down regulation
Pathway Response Notch signaling pathway hsa04330), EGFR tyrosine kinase inhibitor resistance
In-vitro Model PC-9 Lung adenocarcinoma Homo sapiens CVCL_B260
HEK293T Normal Homo sapiens CVCL_0063
HCC827 Lung adenocarcinoma Homo sapiens CVCL_2063
In-vivo Model Control vector, TUSC7 knockout, FLI-06 treated H1975 cells (1*107) cells were suspended in 100 uL of serum-free DMEM medium (Hyclone, USA), mixed with matrix gel (Corning, USA), and then were injected subcutaneously. The changes in the tumor size were recorded every 3 or 5 days.
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: 4920).
Ref 2 M6A associated TSUC7 inhibition contributed to Erlotinib resistance in lung adenocarcinoma through a notch signaling activation dependent way. J Exp Clin Cancer Res. 2021 Oct 16;40(1):325. doi: 10.1186/s13046-021-02137-9.