2. PROTAC MAPK/ERK Pathway Cell Cycle/DNA Damage GPCR/G Protein Apoptosis
  3. Molecular Glues MEK Raf PERK Ras p38 MAPK Apoptosis
  4. 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.

For research use only. We do not sell to patients.

MEK-IN-10

MEK-IN-10 Chemical Structure

CAS No. : 3096958-11-8

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MEK-IN-10 Related Antibodies

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Description

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[1].

IC50 & Target[1]

MEK1

782 nM (IC50)

In Vitro

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.

MEK-IN-10 Related Antibodies

Apoptosis Analysis[1]

Cell Line: AsPC-1, HCT116 and OCI-AML-3 cells
Concentration: 0-100 nM
Incubation Time: 48 h
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.

Cell Cycle Analysis[1]

Cell Line: AsPC-1, HCT116 and OCI-AML-3 cells
Concentration: 0-100 nM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 0, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100 nM
Incubation Time: 4 h
Result: Inhibited p-MEK (IC50 = 0.379 nM) and p-ERK (IC50 = 0.015 nM).

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 3 nM
Incubation Time: 0, 0.25, 1, 4, 8, 24, 48, 72, 96 h
Result: Sustained suppression of both
p-MEK and p-ERK for over 96 h.
Parmacokinetics
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
In Vivo

MEK-IN-10 (1-10 mg/kg, p.o., QOD×21-28) inhibits tumor volume growth in AsPC-1 (KRASG12D) and HCT116 (KRASG13D) model mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AsPC-1 (KRASG12D) model mice[1]
Dosage: 1, 3, 10 mg/kg
Administration: p.o., QOD×28
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.
Animal Model: HCT116 (KRASG13D) model mice[1]
Dosage: 1, 3 mg/kg
Administration: p.o., QOD×21
Result: Significantly inhibited tumor growth with TGI rates of 78% and 86%, respectively at 1 and 3 mg/kg.
Significantly suppressed p-
ERK expression.
Molecular Weight

521.95

Formula

C22H21ClFN5O5S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MEK-IN-10 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MEK-IN-103096958-11-8Molecular GluesMEKRafPERKRasp38 MAPKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KRaf kinasesProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasemouse xenograft modelsRAS-MAPK signaling pathwayHCT116ERKBRAFAsPC-1MEK1OCI-AML-3MIA PaCa-2ras-driven cancersInhibitorinhibitorinhibit

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