2126038-25-1
Chemical Structure
ST-168
- CAS No.: 2126038-25-1
- Formula:C41H44F5IN10O7
- Molecular Weight:1010.75
IUPAC Name: N-(2-(2-(2-(3-(4-(4-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-6-morpholino-1,3,5-triazin-2-yl)piperazin-1-yl)-3-oxopropoxy)ethoxy)ethoxy)ethoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzamide
InChIKey: XIUWBGIKSXLESW-UHFFFAOYSA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
