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SAR405 | SAR405 : Inhibitor of PIK3C3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIK3C3
  • IC50:1 nM
  • Kd:1.5 nM
  • IC50:27 nM
Inhibitor
1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The selectivity of SAR405 was determined in a panel of biochemical assays. SAR405 was found to not b ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Meso Scale electrochemiluminescence technology on phosphorylated Akt
Selectivity Assessment Description:
Selective over class I PI3Ks with IC50s of ∼7 μM and 6 μM for SAR405 in U87MG and PC3 cell lines, re ...

Potency
Cellular
In Vitro

PIK3C3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1681

Chemical Information

Molecular Formula C19H21ClF3N5O2
SMILEs C[C@@H]1COCCN1c1cc(=O)n2c(n1)N(Cc1cncc(Cl)c1)[C@H](C(F)(F)F)CC2
InChI InChI=1S/C19H21ClF3N5O2/c1-12-11-30-5-4-26(12)16-7-17(29)27-3-2-15(19(21,22)23)28(18(27)25-16)10-13-6-14(20)9-24-8-13/h6-9,12,15H,2-5,10-11H2,1H3/t12-,15+/m1/s1
Molecular weight 443.13 Da
AlogP 2.8580000000000014
HBond acceptors 7
HBond donors --
Atoms 51

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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

Expert Reviews

by SERP
(on 12 Aug 2022 )
Cellular Use Rating
Excellent Vsp34 PI3K class III isoform probe for use in the study of autophagy
by SERP+
(on 23 May 2024 )
Cellular Use Rating
The probe has a good in vitro potency, but in cell potency is low. It can be used as a lead compound for further investigation. Also, the cytotoxicity assay was not evaluated.
by SERP+
(on 23 Sept 2024 )
Cellular Use Rating
Very potent compound targeting Vps34 with high selectivy in the lipid kinase family extended to a panel of 200 endogenous kinases.
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