COH-19
COH-19 is a potent mTOR inhibitor. COH-19 binds to the ATP-binding pocket of mTOR, reduces mTOR protein levels, and suppresses the PI3K/Akt/mTOR signaling pathway. COH-19 induces apoptosis via the mitochondrial pathway. COH-19 causes G0/G1 phase cell cycle arrest and suppresses cancer cell proliferation. COH-19 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Formula: C27H17F3N2O2
- Molecular Weight:458.43
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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
COH-19 (24 h) potently inhibits the viability of C6, MG-63, A549, MCF-7, MDA-MB-231 and MCF-10A cells with IC50 values of 18.52, 19.02, 29.02, 17.02, 26.35, and 40.39 μg/mL, respectively[1].
COH-19 (5-25 μg/mL; 24 h) dose-dependently reduces mTOR protein levels in MCF-7 cells[1].
COH-19 (5-25 μg/mL) dose-dependently disrupts membrane integrity in MCF-7 cells, resulting in low cytotoxicity at 5 μg/mL, medium-high cytotoxicity at 10 μg/mL, and high cytotoxicity (80.6%) at 25 μg/mL[1].
COH-19 (15 μg/mL) upregulates pro-apoptotic and tumor suppressor genes (BRCA1, BRCA2, PTEN, TP53, BAX, CASPASE-3, BRAD1) and downregulates PI3K/AKT pathway genes (PI3K, AKT) in MCF-7 cells, while having no significant effect on BCL-2 expression[1].
COH-19 exerts pro-apoptotic effects in MCF-7 cells by increasing BAX and p53 protein levels and decreasing BCL-2 protein levels, while leaving caspase-3 levels unchanged[1].
COH-19 (10-20 μg/mL) induces chromatin decondensation in MCF-7 cells, indicating altered gene expression profiles[1].
COH-19 (10-25 μg/mL) dose-dependently induces apoptosis in MCF-7 cells凋亡[1].
COH-19 binds stably to the ATP-binding pocket of mTOR (PDB ID: 4JT5) with a binding energy of -7.65 kcal/mol[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7
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Concentration:5, 15, 25 μg/mL
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Incubation Time:24 h
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Result:Resulted in mTOR protein levels of 0.4341 ng/mL at 5 μg/mL, 0.2740 ng/mL at 15 μg/mL, and 0.1219 ng/mL at 25 μg/mL.
Caused a statistically significant dose-dependent decrease in mTOR protein levels across the three doses.
Reduced mTOR expression by approximately 86% at the IC50 dose.
Chemical Information
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Molecular Weight 458.43
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Formula C27H17F3N2O2
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SMILES
O=C(C1=CC=C2N=C(C3=CC=C(C4=CC=CC=C4)C=C3)OC2=C1)NC5=CC=C(C(F)(F)F)C=C5
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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