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Imatinib | Imatinib : ATP competitive inhibitor of ABL1, KIT
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ABL1
  • IC 50:38 nM
  • IC 50:100-300 nM
KIT
  • IC 50:100 nM
  • IC 50:100-300 nM
ATP competitive
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
IC50 > 100 uM for many additional kinases, including PKC isoforms, SRC-family kinases, cAMP-dependen ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Imatinib does not interfere with the activity of MAPKs, EGFR, of IGF1R

Potency
Cellular
In Vitro

ABL1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nm0596-561

KIT

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nm0596-561

Orthogonal Probes def

ASCIMINIB
BAFETINIB
GNF-5

Chemical Information

Molecular Formula C29H31N7O
SMILEs Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1
InChI InChI=1S/C29H31N7O/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/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
Molecular weight 493.26 Da
AlogP 4.59032
HBond acceptors 8
HBond donors 2
Atoms 68

Expert Reviews

by SERP
(on 24 May 2016 )
Cellular Use Rating
In Model Organisms
This compound has inadequate selectivity to be considered a probe.
by SERP
(on 6 Jun 2016 )
Cellular Use Rating
In Model Organisms
Imatinib is a non-selective kinase inhibitor originally developed as a tyrosine kinase inhibitor, as shown in several papers (Nature Biotechnology 23, 329 - 336 (2005) ; Nature Biotechnology 26, 127...
by SERP
(on 16 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )

Portal Comments

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(last updated: 7 Nov 2023)

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