Chemical Probes logo
LENIOLISIB | LENIOLISIB : Inhibitor of PIK3CD
RATINGS:
Cellular Use: (1 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIK3CD
  • IC50:11 nM
  • IC50:56 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within protein family: PIK3a 244 nM, PIK3b 424 nM, PIK3g 2230 nM. CDZ173 showed no activ ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Selectivity within protein family: PIK3a 1670 nM, PIK3b 2250 nM

Potency
Cellular
In Vitro

PIK3CD

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acsmedchemlett.7b00293

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.8 h
Systemic clearance: 28 mL/min/kg
Area Under the Curve:: 1355 nM*h
Volume of Distribution at Steady-State: 3.1 L/Kg

DOI Reference: 10.1021/acsmedchemlett.7b00293

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 391 nM
Tmax: 0.4 h
Area Under the Curve:: 1165 nM*h
Bioavailability: 86%

DOI Reference: 10.1021/acsmedchemlett.7b00293

Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 334 nM
Tmax: <0.25 h
Area Under the Curve:: 2107 nM*h
Bioavailability: >100%

DOI Reference: 10.1021/acsmedchemlett.7b00293

Dog
Dose: 0.1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.5 h
Systemic clearance: 2 mL/min/Kg
Area Under the Curve:: 20120 nM*h
Volume of Distribution at Steady-State: 0.3 L/Kg

DOI Reference: 10.1021/acsmedchemlett.7b00293

Dose: 0.3 mg/Kg
Route of delivery: Oral
Cmax: 3410 nM
Tmax: 0.7 h
Area Under the Curve:: 11690 nM*h
Bioavailability: 58%

DOI Reference: 10.1021/acsmedchemlett.7b00293

Monkey (Cynomolgus)
Dose: 0.1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.7 h
Systemic clearance: 17 mL/min/Kg
Area Under the Curve:: 2250 nM*h
Volume of Distribution at Steady-State: 0.6 L/Kg

DOI Reference: 10.1021/acsmedchemlett.7b00293

Dose: 0.3 mg/Kg
Route of delivery: Oral
Cmax: 213 nM
Tmax: <0.5 h
Area Under the Curve:: 297 nM*h
Bioavailability: 13%

DOI Reference: 10.1021/acsmedchemlett.7b00293

Orthogonal Probes def

PI-3065
PICTILISIB

Chemical Information

Molecular Formula C21H25F3N6O2
SMILEs CCC(=O)N1CC[C@H](Nc2ncnc3c2CN(c2cnc(OC)c(C(F)(F)F)c2)CC3)C1
InChI InChI=1S/C21H25F3N6O2/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28)/t13-/m0/s1
Molecular weight 450.20 Da
AlogP 0.0
HBond acceptors 8
HBond donors 1
Atoms 57

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 7 Jul 2022 )
Cellular Use Rating
In Model Organisms
Given the CDZ173 selectivity for PI3K family in the KinomeScan profiling and its superior inhibition of PI3Kdelta in cells (56 nM) compared to the inhibition of PI3Kalpha (1670 nM) and PI3Kbeta (2250 nM),...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria