MEK-IN-10
MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.
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- CAS No.: 3096958-11-8
- Formule: C22H21ClFN5O5S
- Masse moléculaire:521.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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MEK1 782 nM (IC50) |
MEK-IN-10 (D56) potently inhibits the proliferation of AsPC-1, MIA PaCa-2, HCT116, OCI-AML-3 and HT-29 cells, with IC50 values of 0.42, 3.48, 2.27, 0.23 and 2.63 nM[1], respectively.
MEK-IN-10 (0-100 nM; 0-96 h) potently and persistently inhibits p-MEK (IC50 = 0.379 nM) and p-ERK (IC50 = 0.015 nM) in AsPC-1 cells[1].
As a molecular glue, MEK-IN-10 (0.01-10000 nM, 60 min) potently stabilizes the MEK1-BRAF complex (EC50 = 2.37 nM) and MEK1-CRAF complex (EC50 = 11.95 nM) in cell-free TR-FRET assays[1].
MEK-IN-10 (10 nM; 4 h) enhances the formation of the MEK-BRAF complex in HCT116 cells[1].
MEK-IN-10 (1-100 nM, 10 days) inhibits long-term colony formation of HCT116 and AsPC-1 cells in a dose-dependent manner[1].
MEK-IN-10 (0-100 nM; 48 h) induces apoptosis in AsPC-1, HCT116 and OCI-AML-3 cells, and arrests the cells at the G0/G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1, HCT116 and OCI-AML-3 cells
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Concentration:0-100 nM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in apoptotic cells: in AsPC-1 cells, the apoptotic population rose from 7.01% to 17.02%; in HCT116 cells, it rose from 17.08% to 76.0%.
Induced apoptosis in OCI-AML-3 cells.
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Cell Line:AsPC-1, HCT116 and OCI-AML-3 cells
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Concentration:0-100 nM
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Incubation Time:48 h
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Result:Induced dose-dependent accumulation of cells in the G0/G1 phase: in AsPC-1 cells, the G0/G1 population rose from 60.81% to 88.15%; in HCT116 cells, it rose from 42.42% to 75.2%.
Induced G0/G1 phase arrest in OCI-AML-3 cells.
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Cell Line:AsPC-1 cells
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Concentration:0, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100 nM
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Incubation Time:4 h
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Result:Inhibited p-MEK (IC50 = 0.379 nM) and p-ERK (IC50 = 0.015 nM).
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Cell Line:AsPC-1 cells
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Concentration:3 nM
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Incubation Time:0, 0.25, 1, 4, 8, 24, 48, 72, 96 h
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Result:Sustained suppression of both
p-MEK and p-ERK for over 96 h.
| Species | Dose | Route | AUC0-t | MRT0-t | T1/2 | CL | Vss | Cmax | Tmax |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | p.o. | 417.294 μg/L·h | 1.668 h | 1.731 h | 12.228 L/h/kg | 33.921 L/kg | 238.628 μg/L | 0.333 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AsPC-1 (KRASG12D) model mice[1]
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Dosage:1, 3, 10 mg/kg
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Administration:p.o., QOD×28
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Result:Inhibited tumor volume growth in a dose-dependent manne.
Exhibited obvious antitumor effects and the TGI rate was
79% at 10 mg/kg.
Significantly suppressed p-
ERK expression.
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Animal Model:HCT116 (KRASG13D) model mice[1]
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Dosage:1, 3 mg/kg
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Administration:p.o., QOD×21
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Result:Significantly inhibited tumor growth with TGI rates of 78% and 86%, respectively at 1 and 3 mg/kg.
Significantly suppressed p-
ERK expression.
Chemical Information
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CAS No. 3096958-11-8
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Masse moléculaire 521.95
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Formule C22H21ClFN5O5S
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SMILES
NC(C1=C(NC2=C(C=C(C=C2)C=C)F)N(C(C=C1OC3=C(C(NS(=O)(NC)=O)=CC=C3)Cl)=O)C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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