Imatinib

Imatinib : ATP competitive inhibitor of ABL1, KIT

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

ABL1
KIT

ATP competitive

up to 5 uM

More...

Probe Availability:

In Vitro Validations

Uniprot ID: P00519

Target Class: Kinase

Target SubClass: TK

Potency: IC 50

Potency Value: 38 nM

Potency Assay: In vitro assays of protein kinase inhibition

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Tyrosine-protein kinase ABL1, JTK7, ABL, ABL1, ABL ...

DOI Reference: 10.1038/nm0596-561

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

IC50 > 100 uM for many additional kinases, including PKC isoforms, SRC-family kinases, cAMP-dependent kinases, PK, CK1, CK2, EGFR

Probe Selectivity in Cell:

Imatinib does not interfere with the activity of MAPKs, EGFR, of IGF1R

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound has inadequate selectivity to be considered a probe.

(last updated: 24 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 - 132 (2008) ). Imatinib is a potent inhibitior of ABL (Kis in the 10s of nM), DDR1 (Ki=0.8 nM), DDR2 (Ki=15 nM), KIT (Ki=14 nM), LCK (K=40 nM), PDGFRB (Ki=14 nM), PDGFRA (Ki=30 nM) and has affinity for many other kinases (see http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=screens&ligandId=5687). Imatinib also has high affinity for the human quinone reductase 2 (NQO2) (Ki=80 nM; BMC Struct Biol. 2009; 9: 7).

(last updated: 6 Jun 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 16 Mar 2017 )

Portal Comments

In a 2023 study, Hu et al. evaluated Imatinib in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations equal or exceeding 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)