Drug Information

Drug (ID: DG80002) and It's Reported Resistant Information

• Name: Imatinib Mesylate
• Synonyms: Imatinib mesylate|220127-57-1|Gleevec|Glivec|Imatinib mesilate|imatinib methanesulfonate|sti-571|Imatinib accord|Imatinib medac|STI 571|Imatinib (as mesilate)|NSC-716051|QTI-571|Imatinib methane sulfonate|IMKELDI|QTI571|DTXSID9040502|8A1O1M485B|DTXCID7020502|CHEBI:31690|CGP-57148|NSC716051|imatinib oral|Mesylate, Imatinib|RefChem:77|alpha-(4-Methyl-1-piperazinyl)-3'-((4-(3-pyridyl)-2-pyrimidinyl)amino)-p-tolu-p-toluidide|Methanesulfonate, Imatinib|Imatinib mesylate 400 mg|CGP57148B|CGP57148|4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide Monomethanesulfonate|CGP 57148|STI571|Imatinib Mesylate (STI571)|MFCD04307699|Gleevec (Imatinib mesylate)|Imatinib (mesylate)|imatinib monomesylate|N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonate|Imatinib mesylate [USAN]|CGP 57148B|Imatinib mesilate (JAN)|Imatinib mesylate (USAN)|M06311|Imatinib Mesylate(|A form)|Imatinib Methansulfonate|IMATINIB MESILATE [JAN]|CGP-57148B|Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-, methanesulfonate (1:1)|CAS-220127-57-1|220127-57-1 (mesylate)|NCGC00159456-02|Genfatinib|Gleevac|Shantinib|Imatinib, methanesulfonate salt|Gleevec;|4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate|C30H35N7O4S|HSDB 7142|Imatinib mesylate?|4-[(4-Methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate|4-[(4-methylpiperazin-1-yl)methyl]-N-{4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl}benzamide methanesulfonate|Gleevec (TN)|Glivec (TN)|Imatinib mesilate CRS|Imatinib(free base)?|ST-1571 Mesylate|Imatinib Mesylate Tablets|SCHEMBL8217|Imatinib monomethanesulfonate|CHEMBL1642|Benzamide,monomethanesulfonate|Imatinib methanesulfonate salt|MLS001401456|UNII-8A1O1M485B|orb1307991|Imatinib (Mesylate) (Standard)|IMATINIB MESYLATE [HSDB]|SCHEMBL15632914|SCHEMBL29370699|SCHEMBL29377238|EX-A954|IMATINIB MESYLATE [VANDF]|IMATINIB MESILATE [MART.]|YLMAHDNUQAMNNX-UHFFFAOYSA-N|GGP-57148B|GLXC-05064|HMS2052B09|HMS2233D16|HMS3265E01|HMS3265E02|HMS3265F01|HMS3265F02|HMS3372O12|HMS3394B09|HMS3654C07|HMS5079E05|IMATINIB MESILATE [WHO-DD]|Imatinib for system suitability CRS|Tox21_111684|AC-525|HB1943|HY-50946R|s1026|Imatinib mesylate - Bio-X trade mark|IMATINIB METHANESULFONATE [MI]|AKOS015852497|Tox21_111684_1|CCG-101175|FI10812|IMATINIB MESYLATE [ORANGE BOOK]|KS-1236|NC00425|NSC 716051|IMATINIB MESILATE [EP MONOGRAPH]|NCGC00159456-11|111GE005|4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide methanesulfonate|Benzamide, 4-((4-methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)-, monomethanesulfonate|BI164678|HY-50946|methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide|N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonate|SMR000469175|SY013513|I0936|NS00076459|SW197805-4|D01441|Imatinib Mesylate (CGP-57148B, STI-571)|Q27114666|Imatinib Mesylate,Gleevec,Glivec,CGP-57148B,STI-571|4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin- 3-yl)-pyrimidin-2-ylamino)-phenyl]-benzamidemethanesulfonic acid salt|4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benzamide methanesulfonic acid salt|4-[(4-Methyl-1-piperazinyl)-methyl]-N-{4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]-amino]-phenyl}-benzamide monomethanesulphonate|4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate|4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide mesylate|4-[(4-Methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]benzamide methanesulfonate|hydron;methanesulfonate;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide|Methanesulfonic acid--4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide (1/1)|methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl)pyrimidin-2-yl]amino]phenyl]benzamide|N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamidemethanesulfonate
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Chronic myeloid leukemia [ICD-11: 2A20]; [1]
• Formula: 7
• IsoSMILES: InChI=1S/C29H31N7O.CH4O3S/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36;1-5(2,3)4/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34);1H3,(H,2,3,4)
• InChI: CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5.CS(=O)(=O)O
• InChIKey: YLMAHDNUQAMNNX-UHFFFAOYSA-N
• PubChem CID: 123596
• ChEBI ID: CHEBI:31690

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

Chronic myeloid leukemia [ICD-11: 2A20]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: hsa-miR-29a-3p [1]

• Resistant Disease: Chronic myeloid leukemia [ICD-11: 2A20.0]
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Lin-CD34+CD38- cells; Bone; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: Flow cytometry analysis
• Mechanism Description: In particular, the up-regulation of miR-29a-3p and miR-660-5p observed in CML LSCs, led to the down-regulation of their respective targets TET2 and EPAS1 and conferred TKI-resistance to CML LSCs in vitro.

References

• Ref 1: APC Mutations as a Potential Biomarker for Sensitivity to Tankyrase Inhibitors in Colorectal CancerMol Cancer Ther. 2017 Apr;16(4):752-762. doi: 10.1158/1535-7163.MCT-16-0578. Epub 2017 Feb 8.