LDN-211904
Based on 1 publication(s) in Google Scholar
LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC.
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- CAS. Nr.: 1198408-39-7
- Formel: C19H19ClN4O
- Molecular Weight:354.83
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Speicherung:
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Publications Citing Use of MedChemExpress (MCE) LDN-211904
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | CC50 |
>10 μM
Compound: LDN-211904
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Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by alamar blue reagent based analysis
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by alamar blue reagent based analysis
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[PMID: 39028937] |
LDN-211904 (20 μM; 24 h) induces apoptosis by increasing c-PARP in SW48 resistant cells[2].
LDN-211904 (20 μM; 4-20 h) decreases the levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW48 and SW48 Cetuximab-resistant (SW48R) cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced apoptosis by increasing c-PARP.
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Cell Line:SW48 and SW48 Cetuximab-resistant (SW48R) cells
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Concentration:20 μM
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Incubation Time:4 h, 8 h, 20 h
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Result:The levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells were decreased.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells[2]
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Dosage:0.1 mg/kg
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Administration:i.p.; three times a week; for 21 days
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Result:Inhibited tumor growth.
Chemical Information
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CAS. Nr. 1198408-39-7
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Molecular Weight 354.83
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Formel C19H19ClN4O
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SMILES
O=C(C1=CN=C2C=CC(C3CCNCC3)=CN21)NC4=C(Cl)C=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Reinheit & Dokumentation
Verweise
[1]. Qiao L, et al. Structure–activity relationship study of EphB3 receptor tyrosine kinase inhibitors[J]. Bioorganic & medicinal chemistry letters, 2009, 19(21): 6122-6126. [Content Brief]
[2]. Park SH, et al. Sonic hedgehog pathway activation is associated with cetuximab resistance and EPHB3 receptor induction in colorectal cancer. Theranostics. 2019 Apr 12;9(8):2235-2251. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LDN-211904 Related Classifications
HY-136358 Related Classifications
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