2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis
  3. EGFR ERK DNA/RNA Synthesis Apoptosis
  4. 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.

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

Len-604

Len-604 Chemical Structure

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Len-604 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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[1].

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

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.

Len-604 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HUH-7
Concentration: 10, 20 and 30 μM
Incubation Time: 24 h
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%.

Cell Cycle Analysis[1]

Cell Line: HUH-7
Concentration: 10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: HUH-7
Concentration: 10 and 20 μM
Incubation Time: 24 h
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.
In Vivo

Len-604 (5.0 mg/kg; i.v.; once weekly; 14 days) achieves 61.25% tumor growth inhibition in HUH-7 xenograft mice with no observable weight loss[1].
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.

Animal Model: BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
Dosage: 5.0 mg/kg
Administration: i.v.; once weekly; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 61.25%.
Showed no significant mouse weight loss, indicating low systemic toxicity.
Animal Model: BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
Dosage: 15.0 mg/kg; 25.0 mg/kg
Administration: i.v.; once weekly; 21 days
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.
Molecular Weight

880.17

Formula

C30H33ClN8O9Pt
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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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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Len-604 Related Classifications

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Help & FAQs
  • 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:

Len-604Len604Len 604EGFRERKDNA/RNA SynthesisApoptosisEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasesFGFR1ERK phosphorylationFGFR3human hepatocellular carcinoma cell linesFGFR2HUH-7SMMC-7721L02DNA damageFGFR4Inhibitorinhibitorinhibit

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