Drug Information

Drug (ID: DG01466) and It's Reported Resistant Information

• Name: JANEX-1
• Synonyms: JANEX-1; 202475-60-3; WHI-P131; jak3 inhibitor i; Janex 1; 4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol; 4-(6,7-dimethoxyquinazolin-4-ylamino)phenol; 4-((6,7-dimethoxyquinazolin-4-yl)amino)phenol; UNII-1J8Q49TR3I; 1J8Q49TR3I; CHEMBL405130; 4-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenol; 4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol; 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline; 4-((6,7-dimethoxy-4-quinazolinyl)amino)phenol; WHI P131; WHI-P131(Janex 1); Lopac0_001238; SCHEMBL29295; ZINC9851; WHI-P131; JANEX-1; WHI-P 131; WHI-P-131; AOB1974; BCP14722; EX-A2590; 1808AH; BDBM50227519; MFCD01862614; NSC800774; s5903; AKOS002350929; CS-1604; NSC-800774; NCGC00379000-03; AS-35320; HY-15508; QC-11660; 4-(4-hydroxyanilino)-6,7-dimethoxyquinazoline; A925799; J-013147; Phenol, 4-[(6,7-dimethoxy-4-quinazolinyl)amino]-; 4-(4'-Hydroxylphenyl)-amino-6,7-dimethoxyquinazoline hydrochloride dihydrate
• Indication:
  In total 2 Indication(s)
  Heart block [ICD-11: BC63]; Investigative; [1]
  Melanoma [ICD-11: 2C30]; Investigative; [1]
• Target: Adrenergic receptor beta-1 (ADRB1); ADRB1_HUMAN; [1]
• Target: Adrenergic receptor beta-2 (ADRB2); ADRB2_HUMAN; [1]
• Target: Interleukin-12 beta (IL12B); IL12B_HUMAN; [1]
• Formula: 4
• IsoSMILES: COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)O)OC
• InChI: InChI=1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-3-5-11(20)6-4-10/h3-9,20H,1-2H3,(H,17,18,19)
• InChIKey: HOZUXBLMYUPGPZ-UHFFFAOYSA-N
• PubChem CID: 3794
• TTD Drug ID: D0I8FI

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Tyrosine-protein kinase JAK3 (JAK3) [1]

• Molecule Alteration: Missense mutation; p.I87T (c.260T>C)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• Experiment for Molecule Alteration: Immunoblotting analysis
• Experiment for Drug Resistance: CCK-8 assay
• Mechanism Description: The missense mutation p.I87T (c.260T>C) in gene JAK3 cause the sensitivity of JANEX-1 by aberration of the drug's therapeutic target

References

• Ref 1: Functional analysis of JAK3 mutations in transient myeloproliferative disorder and acute megakaryoblastic leukaemia accompanying Down syndromeBr J Haematol. 2008 May;141(5):681-8. doi: 10.1111/j.1365-2141.2008.07081.x. Epub 2008 Apr 7.