TargetMol

ST-168

Product Code:
 
TAR-T28862
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement in MEK1 inhibition respectively, as compared to a previous lead ST-162 in in vitro enzymatic inhibition assays. ST-168 demonstrated superior tumoricidal efficacy over ST-162 in an A375 melanoma spheroid tumor model.
CAS:
T28862
Molecular Weight:
1010.76
Purity:
0.98
SMILES:
O=C(NOCCOCCOCCOCCC(N1CCN(C2=NC(N3C(C(F)F)=NC4=CC=CC=C34)=NC(N5CCOCC5)=N2)CC1)=O)C6=CC=C(F)C(F)=C6NC7=CC=C(I)C=C7F

References

Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168) Marcian E. Van Dort, Stefanie Galb?n, Charles A. Nino, Hao Hong, April A. Apfelbaum, Gary D. Luker, Greg M. Thurber, Lydia Atangcho, Cagri G. Besirli, and Brian D. Ross Publication Date (Web): July 24, 2017 (Letter) doi: 10.1021/acsmedchemlett.7b00111