Drug Information

Drug (ID: DG01637) and It's Reported Resistant Information

• Name: G-749
• Synonyms: G-749; 1457983-28-6; G749; UNII-B06W426B66; 8-bromo-2-[(1-methylpiperidin-4-yl)amino]-4-(4-phenoxyanilino)-6H-pyrido[4,3-d]pyrimidin-5-one; B06W426B66; 8-Bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-D]pyrimidin-5(6H)-one; C25H25BrN6O2; GTPL8108; CHEMBL4544478; SCHEMBL15265027; AOB87764; BCP11201; EX-A1074; 2183AH; MFCD28167815; s7545; ZINC95644293; AKOS026750566; CCG-269863; CS-3343; NCGC00386412-04; AC-33000; BS-15433; DA-33613; HY-12333; QC-11719; FT-0700207; G 749; G 749;G749; A14214; A899265; J-690186; Q27077763; 8-bromo-2-[(1-methylpiperidin-4-yl)amino]-4-[(4-phenoxyphenyl)amino]-5H,6H-pyrido[4,3-d]pyrimidin-5-one
• Indication:
  In total 1 Indication(s)
  Discovery agent [ICD-11: N.A.]; Approved; [1]
• Target: Tyrosine-protein kinase Mer (MERTK); MERTK_HUMAN; [1]
• Formula: 6
• IsoSMILES: CN1CCC(CC1)NC2=NC3=C(C(=O)NC=C3Br)C(=N2)NC4=CC=C(C=C4)OC5=CC=CC=C5
• InChI: InChI=1S/C25H25BrN6O2/c1-32-13-11-17(12-14-32)29-25-30-22-20(26)15-27-24(33)21(22)23(31-25)28-16-7-9-19(10-8-16)34-18-5-3-2-4-6-18/h2-10,15,17H,11-14H2,1H3,(H,27,33)(H2,28,29,30,31)
• InChIKey: SXWMIXPJPNCXQQ-UHFFFAOYSA-N
• PubChem CID: 78357765

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 Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) [1]

• Molecule Alteration: Missense mutation; p.D835Y (c.2503G>T)
• Sensitive Disease: Hematologic Cancer [ICD-11: MG24.Y]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: KG1a cells; Pleural effusion; Homo sapiens (Human); CVCL_1824
• In Vitro Model: Kasumi-1 cells; Peripheral blood; Homo sapiens (Human); CVCL_0589
• In Vitro Model: MOLM-13 cells; Peripheral blood; Homo sapiens (Human); CVCL_2119
• In Vitro Model: MV4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• Experiment for Molecule Alteration: Kinase inhibition assessment assay
• Experiment for Drug Resistance: Fluorometric microculture cytotoxicity assay
• Mechanism Description: The missense mutation p.D835Y (c.2503G>T) in gene FLT3 cause the sensitivity of G-749 by aberration of the drug's therapeutic target

References

• Ref 1: The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemiaBlood Cancer J. 2012 Aug 3;2(8):e81. doi: 10.1038/bcj.2012.28.