Drug Information

Drug (ID: DG01575) and It's Reported Resistant Information

• Name: Gandotinib
• Synonyms: GANDOTINIB; 1229236-86-5; LY2784544; LY 2784544; LY-2784544; UNII-ANC71R916O; Gandotinib (LY2784544); 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine; ANC71R916O; 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine; C23H25ClFN7O; 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine; Gandotinib [USAN:INN]; LY2784544(Gandotinib); Gandotinib (USAN); LY2784544;Gandotinib; Gandotinib(LY2784544); Gandotinib; LY2784544; 3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine; GTPL7909; SCHEMBL2513132; CHEMBL2107823; SCHEMBL15458955; DTXSID20153789; SYN1196; CHEBI:188757; HMS3655L06; HMS3750I09; AOB87108; BCP02309; EX-A1114; MFCD20482143; NSC764820; s2179; ZINC68245097; AKOS026673949; AKOS037643413; BCP9000875; CCG-269448; CS-0426; DB13040; NSC-764820; QC-8978; SB13346; NCGC00345461-02; NCGC00345461-08; 3-((4-Chloro-2-fluorophenyl)methyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8- (morpholin-4-ylmethyl)imidazo(1,2-b)pyridazin-6-amine; 3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8- (morpholinomethyl)imidazo(1,2-b)pyridazin-6-amine; AC-32810; AS-16329; HY-13034; Imidazo(1,2-b)pyridazin-6-amine, 3-((4-chloro-2-fluorophenyl)methyl)-2-methyl-N-(5- methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)-; FT-0700131; SW219960-1; X7498; A25226; D10365; J-511428; Q27077770; 3-[(4-chloro-2-luorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine; Gandotinib;3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine; Imidazo[1,2-b]pyridazin-6-amine, 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)-
• Indication:
  In total 2 Indication(s)
  Myeloproliferative neoplasm [ICD-11: 2A22]; Approved; [1]
  Breast cancer [ICD-11: 2C60]; Phase 1; [1]
• Target: Janus kinase 2 (JAK-2); JAK2_HUMAN; [1]
• Formula: 6
• IsoSMILES: CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F
• InChI: InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)
• InChIKey: SQSZANZGUXWJEA-UHFFFAOYSA-N
• PubChem CID: 46213929
• DrugBank ID: DB13040

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

Myeloproliferative neoplasm [ICD-11: 2A22]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

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

• Molecule Alteration: Missense mutation; p.V617F (c.1849G>T)
• Sensitive Disease: Myeloproliferative neoplasm [ICD-11: 2A22.0]
• Experimental Note: Identified from the Human Clinical Data

References

• Ref 1: A phase 1 study of the Janus kinase 2 (JAK2)(V617F) inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemiaLeuk Res. 2017 Oct;61:89-95. doi: 10.1016/j.leukres.2017.08.010. Epub 2017 Aug 31.