Arf1-GEFs-IN-1
Arf1-GEFs-IN-1 is a potent and orally active ADP-ribosylation factor 1- guanine nucleotide exchange factors (Arf1-GEFs) inhibitor with an IC50 value of 40.85 μM against CT26 cells. Arf1-GEFs-IN-1 primarily mediates tumor regression by triggering anti-tumor immune responses, rather than through direct cytotoxicity. Arf1-GEFs-IN-1 effectively promotes CCL5 expression, demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 can be used for the study of colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 3091068-95-7
- Formula: C19H18N6S
- Molecular Weight:362.45
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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
Arf1-GEFs-IN-1 (Compound 18a) exhibits superior tumor suppression (80.7%) in CT26 cells and demonstrates a much-improved safety profile, with an IC50 of 193.6 μM on 3T3 cells[1].
Arf1-GEFs-IN-1 (2-50 μM) does not directly activate T cells, but instead exerts its effects by modulating the immune microenvironment through tumor cells, likely enhancing its immunogenicity through Arf1 inhibition in CT26 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Arf1-GEFs-IN-1 (5 mg/kg, p.o., for 2 weeks) significantly inhibits tumor growth in CT26 colon cancer xenograft model in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CT26 colon cancer xenograft model in in BALB/c background mice, littermate mice[1]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), for 2 weeks
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Result:The tumor growth inhibition rate percentage (TGI rate%) after treatment was 77.6 %.
No body weight loss was observed.
Be safe, with no significant weight loss or organ damage observed at 300 mg/kg.
Chemical Information
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CAS No. 3091068-95-7
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Molecular Weight 362.45
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Formula C19H18N6S
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SMILES
CN1CCC2=C(SC3=NC=NC(N/N=C/C4=CC5=C(NC=C5)C=C4)=C32)C1
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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
[1]. Li N, et al. Design, synthesis and biological evaluation of (E)-4-(2-((1H-indol-5-yl) methylene) hydrazineyl)-5,6,7,8-tetrahydropyrido [4',3':4,5] thieno[2,3-d] pyrimidine derivatives as Arf1-GEFs inhibitors for the treatment of colon cancer. Eur J Med Chem. 2025 Nov 5;297:117962. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Arf1-GEFs-IN-1 Related Classifications
HY-175290 Related Classifications
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