How effective is compound 50 against cancer?

Introduction

The effectiveness of compound 50 (FN-1501) against cancer has been explored in various research studies, particularly focusing on its potential as a therapeutic agent for acute myeloid leukemia (AML). This synthesis aims to consolidate the key findings from multiple research papers to provide a comprehensive understanding of compound 50's anticancer efficacy.

Key Insights

Potent Inhibitory Activity and Antiproliferative Effects:
- Compound 50 exhibits strong inhibitory activities against FLT3, CDK2, CDK4, and CDK6 with IC50 values in the nanomolar range. It shows significant antiproliferative activities against MV4-11 cells, with an IC50 of 0.008 μM, indicating its potential to suppress cancer cell growth effectively.
Mechanism of Action:
- The compound's mechanism involves the suppression of retinoblastoma phosphorylation, FLT3, ERK, AKT, and STAT5, leading to the induction of apoptosis in cancer cells. This multi-targeted approach enhances its effectiveness against AML.
In Vivo Efficacy:
- In mouse models, compound 50 demonstrated the ability to induce tumor regression at a dose of 15 mg/kg, which is more efficient than the commonly used chemotherapeutic agent cytarabine (50 mg/kg). This highlights its potential for higher efficacy in vivo.
Safety Profile:
- Acute-toxicity studies in mice show that compound 50 has a higher safety margin (LD50: 186 mg/kg) compared to AT7519 (32 mg/kg), suggesting it may be a safer option for therapeutic use.

Conclusion

Compound 50 (FN-1501) shows significant promise as an anticancer agent, particularly for acute myeloid leukemia. It exhibits potent inhibitory and antiproliferative activities, a multi-targeted mechanism of action leading to apoptosis, effective tumor regression in vivo, and a favorable safety profile. These findings collectively support its potential for further development into a therapeutic drug for AML.

How effective is compound 50 against cancer?

Summary

Introduction

Key Insights

Conclusion

Sources and full results

Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.

Compound 50 (FN-1501) shows potential as a safe and efficient acute-myeloid leukemia drug, with potential for further development as a therapeutic agent against acute myeloid leukemia.

BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Compound 11 (BI-97C1), an optically pure Apogossypol derivative, shows potential as a pan-Bcl-2 antagonist and inhibitor of cancer cell growth, offering a potential drug lead for apoptosis-based cancer therapies.

Synthesis of α,β-Unsaturated Carbonyl-Based Compounds, Oxime and Oxime Ether Analogs as Potential Anticancer Agents for Overcoming Cancer Multidrug Resistance by Modulation of Efflux Pumps in Tumor Cells.

Novel,-unsaturated carbonyl-based compounds show potential as anticancer agents and MDR reversal agents by modulating efflux pumps in tumor cells.

Synthesis of Tamoxifen‐Artemisinin and Estrogen‐Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer

Hybrid compounds based on tamoxifen, estrogens, and artemisinin show strong anticancer activity against breast and prostate cancer cell lines, with the most potent being estrogen-artemisinin hybrids 27 and 28 against prostate cancer.

Abstract 1254: Novel acetal and halogen oridonin analogues potently induce apoptosis in prostate cancer cell linesviainduction of p53/p73 and PUMA expression

Novel acetal and halogen oridonin analogues show improved potency against prostate cancer cell growth, with compound 10 showing potential as a novel apoptosis inducer for treatment.

Texas Native Plants Yield Compounds with Cytotoxic Activities against Prostate Cancer Cells.

Texas native plants yield compounds with cytotoxic activities against prostate cancer cells, offering potential new treatments for late-stage and metastatic prostate cancers.

Novel 1,3-Thiazole Analogues with Potent Activity against Breast Cancer: A Design, Synthesis, In Vitro, and In Silico Study

Compound 4 shows potent anti-breast cancer activity, with potential for development into potent anti-breast cancer compounds by targeting VEGFR2 proteins.

The synthetic compound CC-5079 is a potent inhibitor of tubulin polymerization and tumor necrosis factor-alpha production with antitumor activity.

CC-5079 effectively inhibits cancer cell growth and TNF-alpha production, offering potential for neoplastic and inflammatory disease therapy.

An Information-Intensive Approach to the Molecular Pharmacology of Cancer

This study uses a unique compound activity pattern and molecular structural features to explore potential targets and modulators of anticancer activity in cancer cells, potentially generating new clinically active agents.

Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.

Novel VEGFR-2 inhibitors show promising antiproliferative activity against cancer cell lines, with compound 23 showing better antiproliferative activity and comparable safety compared to FDA-approved drugs sorafenib and sunitinib.

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