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PEXIDARTINIB | PEXIDARTINIB : ATP competitive of CSF1R
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
CSF1R
  • IC50:13 nM
  • IC50:8.5 nM
ATP competitive
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
KIT

Gene ID: P10721

Organism: Homo sapiens

Family: Tyr protein kinase family

Potency: IC50 - 27 nM

Potency Assay Off-Target:
SelectScreen profiling Invitrogen of 227 kinases was carried out showing the following IC50s (uM): ...

Potency
Cellular
In Vitro

CSF1R

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1056/NEJMoa1411366

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.5 h
Systemic clearance: 1.77 mL/min/kg
Area Under the Curve:: 9410 hr*ng/mL
Volume of Distribution at Steady-State: 0.33 L/Kg

DOI Reference: 10.1056/NEJMoa1411366

Dose: 5 mg/Kg
Route of delivery: Oral
Cmax: 5590 ng/mL
Area Under the Curve:: 43300 hr*ng/mL
Bioavailability: 92%

DOI Reference: 10.1056/NEJMoa1411366

Dose: 50 mg/Kg
Route of delivery: Oral
Cmax: 35800 ng/mL
Area Under the Curve:: 449000 hr*ng/mL
Bioavailability: 95%

DOI Reference: 10.1056/NEJMoa1411366

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 5.1 h
Systemic clearance: 2.74 mL/min/Kg
Area Under the Curve:: 6450 hr*ng/mL
Volume of Distribution at Steady-State: 1.00 L/Kg

DOI Reference: 10.1056/NEJMoa1411366

Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 10200 ng/mL
Area Under the Curve:: 83100 hr*ng/mL
Bioavailability: 43%

DOI Reference: 10.1056/NEJMoa1411366

Dog
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.9 h
Systemic clearance: 7.75 mL/min/Kg
Area Under the Curve:: 2270 hr*ng/mL
Volume of Distribution at Steady-State: 1.06 L/Kg

DOI Reference: 10.1056/NEJMoa1411366

Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 2980 ng/mL
Area Under the Curve:: 54900 hr*ng/mL
Bioavailability: 81%

DOI Reference: 10.1056/NEJMoa1411366

Monkey (Cynomolgus)
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.7 h
Systemic clearance: 5.86 mL/min/Kg
Area Under the Curve:: 2870 hr*ng/mL
Volume of Distribution at Steady-State: 1.95 L/Kg

DOI Reference: 10.1056/NEJMoa1411366

Dose: 160 mg/Kg
Route of delivery: Oral
Cmax: 29100 ng/mL
Area Under the Curve:: 237000 hr*ng/mL
Bioavailability: 51%

DOI Reference: 10.1056/NEJMoa1411366

Orthogonal Probes def

Vimseltinib
BLZ945

Chemical Information

Molecular Formula C20H15ClF3N5
SMILEs FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1
InChI InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)
Molecular weight 417.10 Da
AlogP 5.228000000000002
HBond acceptors 5
HBond donors 2
Atoms 44

References

Publications

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Expert Reviews

by SERP
(on 18 Oct 2022)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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