Drug Information

Drug (ID: DG00544) and It's Reported Resistant Information

• Name: Erlotinib HCI
• Synonyms: Erlotinib hydrochloride; 183319-69-9; erlotinib HCl; Tarceva; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride; OSI-774; OSI 774; Erlotinib (Hydrochloride); CP 358774; CP-358774; UNII-DA87705X9K; erlotinib, hydrochloride salt; Erlotinib HCl (OSI-744); Tarceva (Erlotinib Hydrochloride); NSC 718781; DA87705X9K; 6,7-bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hydrochloride; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride; MFCD07781272; 4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-, hydrochloride (1:1); NSC-718781; 6,7-bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hcl; 183319-69-9 (HCl); CP-358,774-01; C22H24ClN3O4; [6,7-BIS-(2-METHOXY-ETHOXY)-QUINAZOLIN-4-YL]-(3-ETHYNYL-PHENYL)-AMINE HYDROCHLORIDE; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine Monohydrochloride.; CHEBI:53509; OSI-744; SMR002529980; NSC718781; 4-(m-Ethynylanilino)-6,7-bis(2-methoxyethoxy)quinazoline monohydrochloride; RG-1415; 183319-69-9 pound not183321-74-6; R-1415; Erlotinib, HCl; erlotinib hcl salt; Erlotinib hydrochloride [USAN:INN]; Tarceva (OSI); tarceva hydrochloride; erlotonib hydrochloride; Erlotinib hydrochlroide; Erlotinib(OSI-744); MLS003899192; MLS004774139; C22H23N3O4.HCl; CHEMBL1079742; NSC 718781) HCl; DTXSID10171412; EX-A064; SYN1039; Erlotinib Hydrochloride (Tarceva); BCPP000238; AOB87784; BCP02600; AC-400; CP-358; s1023; AKOS015849087; BCP9000658; CCG-269002; CS-0123; KS-1202; MCULE-9498970160; PB30965; SB16917; 4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-, monohydrochloride; Ro-50-8231; BE164421; BP-30224; HY-12008; M375; (CP358774; DB-011534; AM20090622; FT-0651479; EC-000.2313; CP-358774-01; E-4007; J10200; 319E699; Q27124083; F0001-2385; Erlotinib Hydrochloride,CP-358774, OSI-774, NSC 718781; 6,7-Bis-(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hydrochloride; [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl- phenyl)amine hydrochloride; N-(3-Ethynylphenyl)-6,7-bis(1-methoxyethoxy)-4-quinazolinamine hydrochloride; N-(3-ETHYNYLPHENYL)-6,7-BIS(2-METHOXYETHOXY)-4-QUINAZOLINAMINE HYDROCHLORIDE; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, monohydrochloride; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-quinazolin-4-amine hydrochloride
• Indication:
  In total 3 Indication(s)
  Colon cancer [ICD-11: 2B90]; Phase 2; [1]
  Lung cancer [ICD-11: 2C25]; Approved; [1]
  Pancreatic cancer [ICD-11: 2C10]; Phase 3; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Chordoma [ICD-11: 2B5J]; [2]
• Target: .; NOUNIPROTAC; [2]
• Formula: C22H24ClN3O4
• IsoSMILES: COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl
• InChI: 1S/C22H23N3O4.ClH/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);1H
• InChIKey: GTTBEUCJPZQMDZ-UHFFFAOYSA-N
• PubChem CID: 176871
• INTEDE ID: DR0603

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Chordoma [ICD-11: 2B5J]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Y-box-binding protein 1 (YBX1) [2]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Chordoma [ICD-11: 2B5J.0]
• Experimental Note: Identified from the Human Clinical Data
• Cell Pathway Regulation: EGFR/AKT signaling pathway; Regulation; hsa04012
• Cell Pathway Regulation: Cell invasion; Activation; hsa05200
• In Vitro Model: Chordoma tissue; N.A.
• In Vivo Model: NOD/SCID/IL2Rgamma null (NOG) mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CCK-8 assay
• Mechanism Description: YBX1 regulated protein expression of pEGFR, pAKT and its downstream target genes that influenced cell apoptosis, cell cycle transition and cell invasion. YBX1 activated the EGFR/AKT pathway in chordoma and YBX1-induced elevated expression of key molecules in the EGFR/AKT pathway were downregulated by EGFR and AKT pathway inhibitors. These in vitro results were further confirmed by in vivo data. These data showed that YBX1 promoted tumorigenesis and progression in spinal chordoma via the EGFR/AKT pathway. YBX1 might serve as a prognostic and predictive biomarker, as well as a rational therapeutic target, for chordoma.

References

• Ref 1: Circular RNA hsa_circ_0004015 regulates the proliferation, invasion, and TKI drug resistance of non-small cell lung cancer by miR-1183/PDPK1 signaling pathway. Biochem Biophys Res Commun. 2019 Jan 8;508(2):527-535. doi: 10.1016/j.bbrc.2018.11.157. Epub 2018 Nov 30.
• Ref 2: Y-box binding protein-1 promotes tumorigenesis and progression via the epidermal growth factor receptor/AKT pathway in spinal chordoma .Cancer Sci. 2019 Jan;110(1):166-179. doi: 10.1111/cas.13875. Epub 2018 Dec 19. 10.1111/cas.13875