Imatinib

Protein target name:

BCR-ABL, PDGFR, KIT

Mechanism of action:

ATP-competitive inhibitor

Recommended Concentration for use in cells:

up to 5 uM

Probe Availability

MedChem Express (152459-95-5)

MilliporeSigma (220127-57-1)

Tocris (220127-57-1)

Abcam (220127-57-1)

Cayman (220127-57-1)

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

HUGO ID:

HGNC:76 HGNC:6342

Entrez gene ID:

25 3815

UNIPROT ID:

P00519 P10721

Target alias:

BCR-ABL

Probe Details

Chemical Probes Portal ID:

CPP72

Probe alias:

STI571, CGP 57148

PubChem CID:

5291

ChEMBL ID:

CHEMBL941

SMILES string:

CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

InChi Key:

KTUFNOKKBVMGRW-UHFFFAOYSA-N

Orthogonal probe:

GNF-5BafetinibAsciminib

PAINs evaluation:

PAINs free

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

ABL 38 nM, KIT 100 nM

Off target activity

Potency assay (off target):

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

In cell validation

On target activity in cells

Potency in cells:

IC50

100-300 nM

Potency assay (cells):

Imatinib inhibits autophosphorylation of ABL and PDGFR as well as substrate phosphorylation by KIT

Target engagement assay (cells):

Indirect: inhibition of autophosphorylation or substrate phosphorylation

Off target activity in cells

Potency assay, off target (cells):

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

Primary Reference

Reference (doi):

10.1038/nm0596-561

Reference (PMID):

10910906 8548747 8616716

External Resources

Available data:

GDSC

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB 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...). Imatinib also has high affinity for the human quinone reductase 2 (NQO2) (Ki=80 nM; BMC Struct Biol. 2009; 9: 7).

Jun 12 2016 - 1:44pm

This compound has inadequate selectivity to be considered a probe.

Jun 12 2016 - 1:44pm

Imatinib

Probe Availability

Probe Information

Target Details

BCR-ABL

Probe Details

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

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Imatinib

Probe Availability

Probe Information

Target Details

BCR-ABL

Probe Details

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?