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G749 | G749 : ATP competitive inhibitor of FLT3
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
FLT3 (Mutant:WT, ITD, ITD/N676D, ITD/F691L, D835Y/N676D, D835Y)
  • IC50:0.4 nM FLT3-WT, 0.6 nM FLT3-D835Y
  • IC50:WT 6.1 ± 0.4 nM; ITD 11.8 ± 3.7 nM; ITD/N676D 21.4 ± 1.1 nM; ITD/F691L 38.1 ± 6.6 nM; D835Y/N676D 2.1 ± 0.7 nM; D835Y 3.1 ± 0.5 nM
ATP competitive
up to 10 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - Mer 1 nM , Aurora B 6 nM, RET 9 nM , VEGFR1/FLT1 18 nM, Fms 19 nM , Axl 20 nM , Aurora C 24 nM , FGFR1 25 nM, FGFR3 30 nM, VEGFR2/KDR 39 nM, c-Kit 142 nM

Potency Assay Off-Target:
TR-FRET
Selectivity Assessment Description:
IGF-1R, PDGFRα, PDGFRβ IC50 > 300 nM

Potency
Cellular
In Vitro

FLT3 (Mutant:WT, ITD, ITD/N676D, ITD/F691L, D835Y/N676D, D835Y)

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1182/blood-2013-04-493916

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral

Reference: --

Orthogonal Probes def

QUIZARTINIB

Chemical Information

Molecular Formula C25H25BrN6O2
SMILEs CN1CCC(Nc2nc(Nc3ccc(Oc4ccccc4)cc3)c3c(=O)[nH]cc(Br)c3n2)CC1
InChI InChI=1S/C25H25BrN6O2/c1-32-13-11-17(12-14-32)29-25-30-22-20(26)15-27-24(33)21(22)23(31-25)28-16-7-9-19(10-8-16)34-18-5-3-2-4-6-18/h2-10,15,17H,11-14H2,1H3,(H,27,33)(H2,28,29,30,31)
Molecular weight 520.12 Da
AlogP 5.122600000000004
HBond acceptors 8
HBond donors 3
Atoms 59

References

Publications

Cross References

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Vendors

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Expert Reviews

by SERP
(on 4 Jun 2021 )
Cellular Use Rating
G749 is a highly potent FLT3 kinase inhibitor that also has good activity against mutations such as D835Y and ITD/F691L that confer resistance to AC220. It has good oral bioavailability. However, its...
by SERP
(on 14 Jun 2021 )
Cellular Use Rating
In Model Organisms
This is a high-quality reagent but should be recognized as a dual Flt3/MerTK inhibitor. However, there are other compounds, such as Gilteritinib, an FDA-approved Flt3 inhibitor with a similar kinome...
by SERP
(on 26 Jul 2021 )
Cellular Use Rating
In Model Organisms
The kinase selectivity of this compound is insufficient to make it a good probe, and especially the potent Mer and Aurora B activity are concerning and potentially contribute to the antiproliferative...
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