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NVP-AEW541 | Inhibitor of IGF1R
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
IGF1R
  • IC50:150 nM
  • IC50:86 nM
Inhibitor
Up to 200 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - Ins-R 140 nM, TEK 530 nM, FLT1 600 nM, FLT3 420 nM

Potency Assay Off-Target:
NVP-AEW541 was at least 10-fold selective for IGF1R over all kinases tested except those listed.
In Cell Selectivity Assessment

Potency: IC50 - Ins-R 2.3 uM

Potency Assay Off-Target:
NVP-AEW541 is 27-fold selective for inhibition of IGF1R autophosphorylation > Ins-R autophosphorylat ...

Potency
Cellular
In Vitro

IGF1R

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/S1535-6108(04)00051-0

In Vivo Validations

Mouse
Dose: 20-50 mg/kg
Route of delivery: Oral
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of protein substrate phosphorylation in xenograft tissue

DOI Reference: 10.1016/S1535-6108(04)00051-0

Chemical Information

Molecular Formula C27H29N5O
SMILEs Nc1ncnc2c1c(-c1cccc(OCc3ccccc3)c1)cn2C1CC(CN2CCC2)C1
InChI InChI=1S/C27H29N5O/c28-26-25-24(21-8-4-9-23(14-21)33-17-19-6-2-1-3-7-19)16-32(27(25)30-18-29-26)22-12-20(13-22)15-31-10-5-11-31/h1-4,6-9,14,16,18,20,22H,5,10-13,15,17H2,(H2,28,29,30)
Molecular weight 439.24 Da
AlogP 4.916300000000004
HBond acceptors 6
HBond donors 2
Atoms 62

Vendors

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Expert Reviews

by SERP
(on 9 Jun 2016)
Cellular Use Rating
In Model Organisms
This compound is a potent inhibitor of IGF-1R with cellular activity. Even though the compound has been screened against only a small number of other kinases, it shows some off-target activity, at least...
by SERP
(on 10 Sept 2016)
Cellular Use Rating
In Model Organisms
This probe is suggested to be selective ATP-competitive inhibitor of IGF-1R, and to the lesser extent IR. The original paper (Cancer Cell. 2004 Mar;5(3):231-9) reports a 150 nM IC50 for IGF-1R and 140...
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. Read more about our evaluation criteria