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BAY-293 | BAY-293 : Inhibitor of SOS1
RATINGS:
Cellular Use: (1 reviews)

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

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Targets Biochemical/Biophysical Potency Cellular Potency
SOS1
  • IC50:21 nM
  • IC50:< 1000 nM
  • IC50:< 1000 nM
20 - 1100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Within target family: GEFs: IC50 > 20000 nM on SOS2 and MCF2L (DBS). Selectivity outside target fam ...

Potency
Cellular
In Vitro

SOS1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1073/pnas.1812963116

Negative Control Compounds

BAY-294
Notes: IC50 (SOS1 interaction assay) = 2340 nM (> 100 fold); Shows activity on various targets in the GPCR scan: Closest off-targets are: HRH2 (Ki = 21.13 nM), HTR2A (Ki = 69.37 nM), HTR2B (Ki = 74.56 nM), HTR1D (Ki = 93.49 nM).

Orthogonal Probes def

BI-3406
MRTX-0902
SOS1-IN-1-15

Chemical Information

Molecular Formula C25H28N4O2S
SMILEs CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1
InChI InChI=1S/C25H28N4O2S/c1-15(24-10-18(14-32-24)19-9-7-6-8-17(19)13-26-3)27-25-20-11-22(30-4)23(31-5)12-21(20)28-16(2)29-25/h6-12,14-15,26H,13H2,1-5H3,(H,27,28,29)/t15-/m1/s1
Molecular weight 448.19 Da
AlogP 5.576420000000005
HBond acceptors 6
HBond donors 2
Atoms 60

Vendors

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Expert Reviews

by SERP
(on 18 Jan 2022)
Cellular Use Rating
BAY-293 is a pan-KRASi compound impairing interaction of the GTP-loading SOS1 with KRAS at the low nanomolar level (IC50 = 21 nM), where SOS1 is the guanine nucleotide exchange factor (GEF) and activator...
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