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AC220 | 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
  • KD:1.6 nM
  • IC50:4.2 nM
Inhibitor
1 nM - 300 nM

Selectivity

In Vitro Selectivity Assessment

Potency: KD

Potency Assay Off-Target:
AC220 was tested in Kinomescan panel of 402 kinases (binding assay) at 10 uM. Kinases that bound AC2 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
AC220 was at least 10-fold selective for FLT3 > KIT, PDGFRA/B, RET, and CSFR1.

Potency
Cellular
In Vitro

FLT3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1182/blood-2009-05-222034

In Vivo Validations

Mouse
Dose: 10 mg/mL
Route of delivery: Oral
Plasma half life: ~4 h
Organ of interest (O): xenograft
Target engagement assay: Inhibition of autophosphorylation in xenograft

DOI Reference: 10.1182/blood-2009-05-222034

Orthogonal Probes def

G749

Chemical Information

Molecular Formula C29H32N6O4S
SMILEs CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCOCC5)ccc34)cc2)no1
InChI InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36)
Molecular weight 560.22 Da
AlogP 5.8565
HBond acceptors 10
HBond donors 2
Atoms 72

Vendors

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Expert Reviews

by SERP
(on 22 May 2016 )
Cellular Use Rating
This probe has a number of targets other than FLT3 and is active at 300 nM in human primary cell assays that do not express FLT3. If used as a target-selective probe in a study, this data should be...
by SERP
(on 23 May 2016 )
Cellular Use Rating
In Model Organisms
AC220 is potent and selective and has good PK characteristics. While activity in certain biochemical assays and cellular assays may be evident as low as 0.1-10 nM, drug-resistant models may require...
by SERP
(on 23 May 2016 )
Cellular Use Rating
In Model Organisms
No nonhuman ortholog potencies were reported. Acute oral dosing in mice was shown be tolerated (up to 300 mg/kg), though PK was linear up through 100 mg/kg. Repeat dosing was only performed at 10 mg/kg....
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