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Vimseltinib | Inhibitor of CSF1R
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
CSF1R
  • IC50:4.2 nM @ 4 mM ATP
  • IC50:19 nM
  • IC50:9.2 nM
Inhibitor
1 µM

Selectivity

In Vitro Selectivity Assessment
KIT

Gene ID: P10721

Organism: Homo sapiens

Family: Tyr protein kinase family

Potency: IC50 - 1600 nM

Potency Assay Off-Target:
Vimseltinib was profiled versus a total of approximately 300 human kinases at 10 mM ATP. Kinases inh ...
Selectivity Assessment Description:
Vimseltinib was >100-fold selective for CSF1R versus all kinases tested and >1,000-fold selective fo ...

Potency
Cellular
In Vitro

CSF1R

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-21-0361

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 11.1 h
Systemic clearance: 0.046 L/h/Kg
Cmax: 10738 ng/mL
Tmax: 6 h
Area Under the Curve:: 170035 ng*h/mL
Volume of Distribution at Steady-State: 0.731 L/Kg

DOI Reference: 10.1158/1535-7163.MCT-21-0361

Dose: 3 mg/Kg
Route of delivery: Oral
Plasma half life: 8.96 h
Systemic clearance: 0.052 L/h/Kg
Cmax: 3226 ng/mL
Tmax: 6 h
Area Under the Curve:: 49314 ng*h/mL
Volume of Distribution at Steady-State: 0.661 L/Kg

DOI Reference: 10.1158/1535-7163.MCT-21-0361

Dose: 1 mg/Kg
Route of delivery: Oral
Plasma half life: 9.07 h
Systemic clearance: 0.057 L/h/Kg
Cmax: 1121 ng/mL
Tmax: 2 h
Area Under the Curve:: 14625 ng*h/mL
Volume of Distribution at Steady-State: 0.744 L/Kg

DOI Reference: 10.1158/1535-7163.MCT-21-0361

Orthogonal Probes def

PEXIDARTINIB
AC710

Chemical Information

Molecular Formula C23H25N7O2
SMILEs Cc1nc(-c2cnc(NC(C)C)n(C)c2=O)ccc1Oc1ccnc(-c2cnn(C)c2)c1
InChI InChI=1S/C23H25N7O2/c1-14(2)27-23-25-12-18(22(31)30(23)5)19-6-7-21(15(3)28-19)32-17-8-9-24-20(10-17)16-11-26-29(4)13-16/h6-14H,1-5H3,(H,25,27)
Molecular weight 431.21 Da
AlogP 0.0
HBond acceptors 9
HBond donors 1
Atoms 57

Vendors

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Expert Reviews

No SERP comments found for Vimseltinib

Probe Vimseltinib is in the process of SERP review.

Please continue to check back for new reviews and commentary.