Drug Information

Drug (ID: DG01548) and It's Reported Resistant Information

• Name: Momelotinib
• Synonyms: Cyt387; 1056634-68-4; MOMELOTINIB; Cyt-387; CYT 387; N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide; CYT 11387; UNII-6O01GMS00P; N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide; Momelotinib (CYT387); N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide; 6O01GMS00P; CHEMBL1078178; CYT11387; N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide; N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)-amino)pyrimidin-4-yl)benzamide; CYT-11387; MFCD16038899; GS-0387; LM-1149; N-(Cyanomethyl)-4-(2-((4-(morpholin-4-yl)phenyl)amino)pyrimidin-4-yl)benzamide; N-(cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)benzamide; Benzamide, N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)-; Momelotinib [USAN:INN]; momelotinibum; benzamide, n-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-; C87; Momelotinib (USAN/INN); MLS006011154; GTPL7791; SCHEMBL2237234; CHEBI:91407; AOB4616; EX-A260; QCR-259; SYN1035; HMS3244K19; HMS3244K20; HMS3244L19; HMS3295I01; HMS3655D12; HMS3744C15; BCP02328; CYT-0387; CYT387, CYT11387; CYT387,CYT 11387; Momelotinib (CYT387,CYT-387); BDBM50311017; NSC767598; NSC800800; s2219; ZINC43199890; AKOS015904624; N-(Cyanomethyl)-4-[2-[(4-morpholinophenyl)amino]-4-pyrimidinyl]benzamide; BCP9000570; CCG-264946; CS-0053; DB11763; LS41099; NSC-767598; NSC-800800; SB14602; NCGC00244257-01; NCGC00244257-08; AC-23162; AS-19389; HY-10961; SMR004702928; SY060668; FT-0755949; SW219679-1; X7506; D10315; A857769; Q252602; J-001468; J-523159; BRD-K87737963-001-01-1; N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide; N-(cyanomethyl)-4-[2-[4-(4-morpholinyl)anilino]-4-pyrimidinyl]benzamide; N-(cyanomethyl)-4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzamide; Benzamide,N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-; N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide;CYT387
• Indication:
  In total 1 Indication(s)
  Endometrial cancer [ICD-11: 2C76]; Phase 3; [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: PI3-kinase gamma (PIK3CG); PK3CG_HUMAN; [1]
• Target: Serine/threonine-protein kinase mTOR (mTOR); MTOR_HUMAN; [1]
• Formula: 6
• IsoSMILES: C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
• InChI: InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
• InChIKey: ZVHNDZWQTBEVRY-UHFFFAOYSA-N
• PubChem CID: 25062766
• ChEBI ID: CHEBI:91407
• TTD Drug ID: D0N5JZ
• VARIDT ID: DR1880
• DrugBank ID: DB11763

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.