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NVL-520 | NVL-520 : Inhibitor of ROS1 and ROS1 G2032R
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
ROS1 (Mutant:WT, G2032R)
  • IC50:0.7 nM
  • IC50:7.9 nM
  • IC50:1.3 nM
  • IC50:3.6 nM
Inhibitor
up to 300 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
In a biochemical screen against 335 wild-type human kinase domains, NVL-520 was highly selective. RO ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Selectivity against TRK family was confirmed via cell viability assay
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Mutagenesis screens: Predicting resistance in a TKI-naïve setting
Selectivity Assessment Description:
Zidesamtinib suppressed ROS1 mutations in ENU mutagenesis screens. (DOI: 10.1158/1535-7163.MCT-25-00 ...

Potency
Cellular
In Vitro

ROS1 (Mutant:WT, G2032R)

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/2159-8290.CD-22-0968

In Vivo Validations

Rat
Dose: 10 mg/Kg
Route of delivery: Oral
Tmax: 84%

DOI Reference: 10.1158/2159-8290.CD-22-0968

Chemical Information

Molecular Formula C22H22FN7O
SMILEs CCn1ncc2c1-c1cnc(N)c(c1)O[C@H](C)c1cc(F)ccc1-c1nn(C)nc1C2
InChI InChI=1S/C22H22FN7O/c1-4-30-21-13(11-26-30)7-18-20(28-29(3)27-18)16-6-5-15(23)9-17(16)12(2)31-19-8-14(21)10-25-22(19)24/h5-6,8-12H,4,7H2,1-3H3,(H2,24,25)/t12-/m1/s1
Molecular weight 419.19 Da
AlogP 3.5260000000000025
HBond acceptors 8
HBond donors 2
Atoms 53

References

Publications

Cross References

canSARChEMBL

Expert Reviews

by SERP
(on 14 Dec 2025 )
Cellular Use Rating
In Model Organisms
The use of this compound as a cellular probe should take into account the nearly equipotent activity on ALK fusion lines and relevant activity in TRKB lines. The recommended dose of 300 nM will be above...
by SERP
(on 21 Jan 2026 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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