LC-MG-10
LC-MG-10 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 230.2 nM in KATO III cells. LC-MG-10 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-10 inhibits cancer cell proliferation. LC-MG-10 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-10 can be used in studies related to gastric cancer.
For research use only. We do not sell to patients.
- Formula: C35H35Cl2N7O6
- Molecular Weight:720.60
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR2 230.2 nM (DC50) |
LC-MG-10 (0-10000 nM; 12 h) potently induces dose-dependent degradation of FGFR2 in KATO III gastric cancer cells, with a DC50 of 230.2 nM[1].
LC-MG-10 (0-1000 nM; 12 h) inhibits FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways in KATO III gastric cancer cells following 12 h of treatment at concentrations of 300 nM and 1000 nM[1].
LC-MG-10 (1 μM; 0-12 h) induces the internalization of FGFR2 from the plasma membrane into intracellular vesicles in KATO III gastric cancer cells[1].
LC-MG-10 (1 μM; 0 h-8 h) induces time-dependent degradation of FGFR2 in KATO III gastric cancer cells[1].
LC-MG-10 (96 h) potently inhibits the proliferation of KATO III gastric cancer cells, with an IC50 value of 49.13 nM[1].
Degradation of FGFR2 in KATO III gastric cancer cells induced by LC-MG-10 (200 nM) depends on the ubiquitin-proteasome system[1].
LC-MG-10 (1 μM; 1 h) binds to the ATP-binding pocket of FGFR2 to mediate its degradation, whereas pre-treatment with the parent inhibitor Infigratinib (HY-13311) blocks this activity in KATO III gastric cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KATO III cells
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Concentration:0, 300, 1000 nM
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Incubation Time:12 h
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Result:Abrogated both the PI3K/AKT and MAPK/ERK signaling cascades, as evidenced by the markedly diminished phosphorylation of the primary docking protein FRS2α (Tyr436), as well as
PLCγ (Tyr783), SHP2 (Tyr524), AKT (Ser473), ERK1/2, and the downstream terminal kinase RSK1 (Thr573).
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Cell Line:KATO III cells
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Concentration:1 μM
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Incubation Time:0, 6, 12 h
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Result:Triggered the rapid relocalization of FGFR2 from the plasma membrane into intracellular vesicular compartments.
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Cell Line:KATO III cells
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Concentration:1 μM
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Incubation Time:0, 1, 2, 4, 8 h
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Result:Induced time-dependent degradation of FGFR2 in KATO III gastric cancer cells, with detectable depletion starting at 4 hours and maximal clearance by 8 hours of treatment with 1 μM.
Chemical Information
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Molecular Weight 720.60
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Formula C35H35Cl2N7O6
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SMILES
O=C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)N(C2=NC=NC(NC3=CC=C(N4CCN(C(/C=C/C(C5=CC=C(OC)C=C5)=O)=O)CC4)C=C3)=C2)C
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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)
LC-MG-10 Related Classifications
HY-184322 Related Classifications
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