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.
For research use only. We do not sell to patients.
- CAS No.: 2126038-25-1
- Formula: C41H44F5IN10O7
- Molecular Weight:1010.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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MEK1 182 nM (IC50) |
PI3Kα 69.2 nM (IC50) |
PI3Kδ 41.7 nM (IC50) |
PI3Kβ 1482 nM (IC50) |
PI3Kγ 2293 nM (IC50) |
Chemical Information
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CAS No. 2126038-25-1
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Molecular Weight 1010.75
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Formula C41H44F5IN10O7
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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