Drug Information

Drug (ID: DG01797) and It's Reported Resistant Information

• Name: N-[(5,7-dichloro-2,3-dihydro-1-benzofuran-2-yl)methyl]propan-2-amine
• Synonyms: NULL
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Breast cancer [ICD-11: 2C60]; [1]
• Target: .; NOUNIPROTAC; [1]
• Formula: 3
• IsoSMILES: CC(C)NCC1CC2=C(O1)C(=CC(=C2)Cl)Cl
• InChI: InChI=1S/C12H15Cl2NO/c1-7(2)15-6-10-4-8-3-9(13)5-11(14)12(8)16-10/h3,5,7,10,15H,4,6H2,1-2H3
• InChIKey: FCFGRTQYVIIVRZ-UHFFFAOYSA-N
• PubChem CID: 36806

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Breast cancer [ICD-11: 2C60]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: HOX transcript antisense RNA (HOTAIR) [1]

• Molecule Alteration: Up-regulation; Interaction
• Resistant Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: MGC-803 cells; Gastric; Homo sapiens (Human); CVCL_5334
• In Vitro Model: SGC-7901 cells; Gastric; Homo sapiens (Human); CVCL_0520
• In Vitro Model: N5 cells; N.A.; .; N.A.
• In Vitro Model: N33 cells; N.A.; Mus musculus (Mouse); CVCL_9417
• In Vitro Model: Cal51 cells; Pleural effusion; Homo sapiens (Human); CVCL_1110
• In Vivo Model: Nude mice model; Mus musculus
• Experiment for Molecule Alteration: RIP experiments; ChIP; QqRT-PCR; Western bloting analysis
• Experiment for Drug Resistance: CCK8 assay
• Mechanism Description: AQB is a HOTAIR-EZH2 inhibitor, which blocks PRC2 recruitment and has great potential as an effective agent for targeted cancer therapy.

References

• Ref 1: A Compound AC1Q3QWB Selectively Disrupts HOTAIR-Mediated Recruitment of PRC2 and Enhances Cancer Therapy of DZNepTheranostics. 2019 Jun 24;9(16):4608-4623. doi: 10.7150/thno.35188. eCollection 2019.