ST-168

ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research[1][2].

Product Specifications

CAS Number

[2126038-25-1]

UNSPSC

12352005

Target

Akt; Apoptosis; Caspase; MEK; PI3K

Related Pathways

Apoptosis; MAPK/ERK Pathway; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C(NOCCOCCOCCOCCC(N1CCN(C2=NC(N3C4=CC=CC=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)=O)C6=CC=C(F)C(F)=C6NC7=CC=C(I)C=C7F

Molecular Formula

C41H44F5IN10O7

Molecular Weight

1010.75

References & Citations

[1]Van Dort ME, et al. Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168) . ACS Med Chem Lett. 2017 Jul 24;8 (8) :808-813.|[2]Smith A, et al. Ocular Toxicity Profile of ST-162 and ST-168 as Novel Bifunctional MEK/PI3K Inhibitors. J Ocul Pharmacol Ther. 2018 Jul/Aug;34 (6) :477-485.