Drug Information

Drug (ID: DG01549) and It's Reported Resistant Information

• Name: AZ960
• Synonyms: 905586-69-8; AZ 960; AZ-960; AZ960; UNII-M63IS9PTJF; (S)-5-Fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile; M63IS9PTJF; (S)-5-fluoro-2-((1-(4-fluorophenyl)ethyl)amino)-6-((5-methyl-1H-pyrazol-3-yl)amino)nicotinonitrile; CHEMBL1774055; 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile; C18H16F2N6; 5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile; 5-fluoro-2-{[(1S)-1-(4-fluorophenyl)ethyl]amino}-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile; MLS006011063; GTPL8476; SCHEMBL14840365; DTXSID60238201; SYN1015; BCPP000371; BCP27683; EX-A1802; AZ 960;AZ960; BDBM50343725; s2214; ZINC43205072; AKOS027420925; BCP9000348; CCG-268082; CS-6209; NCGC00346581-01; NCGC00346581-02; NCGC00346581-04; NCGC00346581-06; 3-Pyridinecarbonitrile, 5-fluoro-2-(((1S)-1-(4-fluorophenyl)ethyl)amino)-6-((5-methyl-1H-pyrazol-3-yl)amino)-; AC-32981; AS-74896; HY-10411; SMR004702855; SW219623-1; X7504; A19389; C77068; 586F698; J-502242; Q27074679; (R)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile; (S)-5-Fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino) nicotinonitrile; (S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile;AZ 960
• Indication:
  In total 3 Indication(s)
  Myelofibrosis [ICD-11: 2A20]; Investigative; [1]
  Polycythemia vera [ICD-11: 2A20]; Investigative; [1]
  Thrombocythemia [ICD-11: 3B63]; Investigative; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Hematologic cancer [ICD-11: MG24]; [1]
• Target: Janus kinase 2 (JAK-2); JAK2_HUMAN; [1]
• Formula: 5
• IsoSMILES: CC1=CC(=NN1)NC2=C(C=C(C(=N2)N[C@@H](C)C3=CC=C(C=C3)F)C#N)F
• InChI: InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1
• InChIKey: SUNXHXDJOIXABJ-NSHDSACASA-N
• PubChem CID: 25099184
• TTD Drug ID: D0D5ZJ

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

Hematologic cancer [ICD-11: 2B3Z]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Tyrosine-protein kinase JAK2 (JAK3) [1]

• Molecule Alteration: Missense mutation; p.R867Q (c.2600G>A)
• Resistant Disease: Hematologic Cancer [ICD-11: MG24.Y]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: WST-1 cell proliferation assay

References

• Ref 1: Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitorsBlood. 2014 Feb 27;123(9):1372-83. doi: 10.1182/blood-2013-05-504555. Epub 2014 Jan 7.