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Pictilisib | Pictilisib : ATP-competitive inhibitor of PIK3CA, PIK3CD
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (4 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
PIK3CA
  • IC 50:3 nM
  • Ki:10.2 nM
  • IC 50:28-46 nM
PIK3CD
  • IC 50:3 nM
  • IC 50:28-46 nM
ATP competitive
10 nM - 500 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PIK3CB 0.033 uM, PIK3CD 0.075 uM, C2 beta 0.67 uM, VPS34 >10 uM, DNA-PK 1.23 uM, MTOR Ki(app) = 0.58 uM

Potency Assay Off-Target:
Scintillation proximity assay
Selectivity Assessment Description:
Kinase Profiler assessment of 228 protein kinases revealed <50% inhibition at 1 uM for all kinases e ...

Potency
Cellular
In Vitro

PIK3CA

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm800295d

PIK3CD

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm800295d

In Vivo Validations

Mouse
Dose: 75 ng/kg
Route of delivery: Oral
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of protein substrate phosphorylation in xenograft tissue

DOI Reference: 10.1021/jm800295d

Orthogonal Probes def

BYL719
APITOLISIB
PI-3065

Chemical Information

Molecular Formula C23H27N7O3S2
SMILEs CS(=O)(=O)N1CCN(Cc2cc3nc(-c4cccc5[nH]ncc45)nc(N4CCOCC4)c3s2)CC1
InChI InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
Molecular weight 513.16 Da
AlogP 0.0
HBond acceptors 10
HBond donors 1
Atoms 62

Vendors

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Expert Reviews

by SERP
(on 2 Jun 2016 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 17 Jun 2016 )
Cellular Use Rating
In Model Organisms
GDC-0941 is an inhibitor of class I PI3 kinases (IC50 α, β, δ, γ = 3, 33, 3, 75 nM, respectively) with selectivity over class II, III and IV enzymes C2β (670 nM), Vps34 (>10 µM), DNA-PK (1.23 µM) and...
by SERP
(on 13 Jul 2016 )
Cellular Use Rating
In Model Organisms
For cell culture, I would recommend confirming class I inhibition without inhibition of the other classes (class II-class IV). However, because cell-free sensitivities of the p110s vary from 3 nM (alpha)...
by SERP
(on 13 Jul 2016 )
Cellular Use Rating
In Model Organisms
Chemical Neighbourhood for QSAR: 129, 47, and 24 molecules similar (>0.80) to GDC-0941 with in vitro affinities for PIK3CA, PIK3CD, and PIK3CB, respectively, were found in public repositories (e.g.,...
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