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PF-06869206 | PF-06869206 : Inhibitor of SLC34A1
RATINGS:
Cellular Use: (2 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
SLC34A1
  • IC50:350 nM
  • IC50:1400 nM
Inhibitor
up to 10 uM

Selectivity

In Cell Selectivity Assessment

Potency: IC50

Selectivity Assessment Description:
NaPi2b, NaPi2c, PiT-1, PiT2, Parental HEK IC50 >25 uM

Potency
Cellular
In Vitro

SLC34A1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acsmedchemlett.8b00013

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 4.8 h
Systemic clearance: 15. mL/min/Kg
Area Under the Curve:: 1100 ng·h/mL
Volume of Distribution at Steady-State: 3.1 L/Kg

DOI Reference: 10.1021/acsmedchemlett.8b00013

Dose: 5 mg/Kg
Route of delivery: Oral
Cmax: 720 ng/mL
Tmax: 0.75 h
Area Under the Curve:: 4800 ng·h/mL
Bioavailability: 87%

DOI Reference: 10.1021/acsmedchemlett.8b00013

Dose: 50 mg/Kg
Route of delivery: Oral
Cmax: 6000 ng/mL
Tmax: 1.0 h
Area Under the Curve:: 77000 ng·h/mL
Bioavailability: 140%

DOI Reference: 10.1021/acsmedchemlett.8b00013

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.75 h
Systemic clearance: 22 mL/min/kg
Area Under the Curve:: 760 ng·h/mL
Volume of Distribution at Steady-State: 0.86 L/Kg

DOI Reference: 10.1021/acsmedchemlett.8b00013

Dose: 5 mg/Kg
Route of delivery: Oral
Cmax: 540 ng/mL
Tmax: 0.38 h
Area Under the Curve:: 1000 ng·h/mL
Bioavailability: 27%

DOI Reference: 10.1021/acsmedchemlett.8b00013

Dose: 50 mg/Kg
Route of delivery: Oral
Cmax: 11000 ng/mL
Tmax: 1.5 h
Area Under the Curve:: 92000 ng·h/mL
Bioavailability: 240%

DOI Reference: 10.1021/acsmedchemlett.8b00013

Chemical Information

Molecular Formula C15H14ClF3N4O2
SMILEs Cc1[nH]c2c(N3CCO[C@H](CO)C3)c(C#N)c(C(F)(F)F)nc2c1Cl
InChI InChI=1S/C15H14ClF3N4O2/c1-7-10(16)11-12(21-7)13(23-2-3-25-8(5-23)6-24)9(4-20)14(22-11)15(17,18)19/h8,21,24H,2-3,5-6H2,1H3/t8-/m0/s1
Molecular weight 374.08 Da
AlogP 2.612700000000001
HBond acceptors 6
HBond donors 2
Atoms 39

References

Publications

Cross References

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Expert Reviews

by SERP
(on 22 Feb 2021 )
Cellular Use Rating
In Model Organisms
The probe is a micromolar inhibitor of the NaPi2a sodium-phosphate cotransporter in cells (direct target engagement is not confirmed). There are limited data describing the selectivity of the probe....
by SERP
(on 26 Feb 2021 )
Cellular Use Rating
In Model Organisms
There are no biochemical assays reported for this target so all inhibition data have been generated in cellular assays. The IC50 value of 0.38 uM was determined in HEK293 cells stably expressing NaPi2a...
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