Len-604
Len-604 is a FGFR inhibitor with IC50 values of 9.71 nM, 9.93 nM, 29.80 nM and 14.48 nM against FGFR4, FGFR1, FGFR2 and FGFR3, respectively. Len-604 reduces the phosphorylation levels of FGFR4 and ERK, and induces DNA damage and apoptosis in cancer cells. Len-604 is applicable to research related to liver cancer.
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- Formule: C30H33ClN8O9Pt
- Masse moléculaire:880.17
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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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ERK1 |
ERK2 |
Len-604 (72 h) exhibits potent cytotoxicity against HUH-7 and SMMC-7721 human hepatocellular carcinoma cells (IC50 = 5.62 μM and 5.64 μM, respectively), and shows high selectivity toward non-cancerous L02 hepatocytes[1].
Len-604 (10-30 μM; 24 h) induces dose-dependent apoptosis in human hepatocellular carcinoma HUH-7 cells, with the apoptosis rate reaching 51.1% after treatment with 30 μM for 24 h[1].
Len-604 (10 μM; 24 h) induces S-phase cell cycle arrest in human hepatocellular carcinoma cell line HUH-7 after 24 h of incubation[1].
Len-604 (10-20 μM; 24 h) downregulates the levels of p-FGFR4 and p-ERK1/2 in human hepatocellular carcinoma cell line HUH-7 in a dose-dependent manner, without altering the protein levels of total FGFR4 and ERK1/2[1].
Len-604 (10 μM; 12-24 h) induces significant DNA damage in human hepatocellular carcinoma cell line HUH-7, as evidenced by elevated γ-H2AX expression levels and DNA strand breaks detected via the comet assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUH-7
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Concentration:10, 20 and 30 μM
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Incubation Time:24 h
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Result:Induced cell apoptosis in a dose-dependent manner.
At 10 μM, showed an apoptotic ratio higher than lenvatinib but lower than cisplatin and the lenvatinib-cisplatin mixture.
At 30 μM, reached an apoptotic ratio of 51.1%.
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Cell Line:HUH-7
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Concentration:10 μM
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Incubation Time:24 h
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Result:Decreased G0-G1 phase cell distribution from 77.7% to 67.5% compared to control.
Increased S-phase distribution from 15.7% to 30.7% compared to control.
Caused S-phase arrest similar to cisplatin and the lenvatinib-cisplatin mixture.
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Cell Line:HUH-7
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Concentration:10 and 20 μM
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Incubation Time:24 h
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Result:Downregulated phosphorylated FGFR4 (p-FGFR4) in a dose-dependent manner.
Downregulated phosphorylated ERK1/2 (p-ERK1/2) in a dose-dependent manner.
Left levels of total FGFR4 and ERK1/2 unchanged.
At 10 μM, showed inhibition of p-FGFR4 nearly equivalent to lenvatinib.
Len-604 (15-25 mg/kg; i.v.; once weekly; 21 days) achieves 64.96% and 91.98% tumor growth inhibition, respectively, in HUH-7 xenograft mice with low systemic toxicity and dose-dependent suppression of FGFR4/ERK signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
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Dosage:5.0 mg/kg
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Administration:i.v.; once weekly; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 61.25%.
Showed no significant mouse weight loss, indicating low systemic toxicity.
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Animal Model:BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
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Dosage:15.0 mg/kg; 25.0 mg/kg
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Administration:i.v.; once weekly; 21 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 64.96% at 15.0 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 91.98% at 25.0 mg/kg.
Showed no significant changes in mouse body weight at both doses.
Revealed no toxic impacts on major organs (heart, liver, spleen, lung, kidney) via histopathological analysis.
Showed severe tumor cell degeneration/necrosis in tumor tissue sections.
Induced dose-dependent downregulation of phosphorylated FGFR4 (p-FGFR4) and phosphorylated ERK1/2 (p-ERK1/2) levels in tumor tissues via Western blot analysis.
Chemical Information
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Masse moléculaire 880.17
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Formule C30H33ClN8O9Pt
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SMILES
O=C(NC1CC1)NC2=C(Cl)C=C(OC3=CC=NC4=C3C=C(C(NCCC(N/N=C5CC6(C([O-][Pt+2]([NH3])([NH3])[O-]C6=O)=O)C\5)=O)=O)C(OC)=C4)C=C2
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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)
Len-604 Related Classifications
HY-182817 Related Classifications
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