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BERZOSERTIB | BERZOSERTIB : Inhibitor of ATR
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
ATR
  • Ki:0.2 nM
  • IC50:19 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
VE-822 (0.4 and 2 μM) was screened against a set of human, rat, mouse and fission yeast kinases usin ...

Potency
Cellular
In Vitro

ATR

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/cddis.2012.181

In Vivo Validations

Mouse
Dose: 60 mg/Kg
Route of delivery: Oral
Target engagement assay: mice bearing subcutaneous COLO205 tumors

DOI Reference: 10.1158/0008-5472.CAN-13-3369

Chemical Information

Molecular Formula C24H25N5O3S
SMILEs CNCc1ccc(-c2cc(-c3nc(-c4ccc(S(=O)(=O)C(C)C)cc4)cnc3N)on2)cc1
InChI InChI=1S/C24H25N5O3S/c1-15(2)33(30,31)19-10-8-18(9-11-19)21-14-27-24(25)23(28-21)22-12-20(29-32-22)17-6-4-16(5-7-17)13-26-3/h4-12,14-15,26H,13H2,1-3H3,(H2,25,27)
Molecular weight 463.17 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 58

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Expert Reviews

No SERP comments found for BERZOSERTIB

Probe BERZOSERTIB is in the process of SERP review.

Please continue to check back for new reviews and commentary.