2. GPCR/G Protein
  3. Arf Family GTPase
  4. 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.

Arf1-GEFs-IN-1

Arf1-GEFs-IN-1 Chemical Structure

CAS No. : 3091068-95-7

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Arf1-GEFs-IN-1 Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

Arf1-GEFs-IN-1 (Compound 18a) shows short half-lives in both mouse liver microsomes (MLM, t1/2 = 31.1 min) and human liver microsomes (HLM, t1/2 = 59.2 min), and lower plasma protein binding in both mouse (94.9%) and human (94.1%) plasma[1].
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.

Animal Model: CT26 colon cancer xenograft model in in BALB/c background mice, litter­mate mice[1]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), for 2 weeks
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.
Molecular Weight

362.45

Formula

C19H18N6S
CAS No.
SMILES

CN1CCC2=C(SC3=NC=NC(N/N=C/C4=CC5=C(NC=C5)C=C4)=C32)C1
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Purity & Documentation
References
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Arf1-GEFs-IN-1 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:

Arf1-GEFs-IN-13091068-95-7Arf Family GTPaseADP-ribosylation Factor (ARF) Family GTPase(E)-hydrazone derivatives of thieno[2,3-d]PyrimidineDrosophila-based phenotypic screenColon cancer immunotherapyInhibitorinhibitorinhibit

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