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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
Vendors
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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

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