ST-168
| Code | Size | Price |
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| TAR-T28862-100mg | 100mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| TAR-T28862-500mg | 500mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Documents
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