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.

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Arf1-GEFs-IN-1

Arf1-GEFs-IN-1 Chemical Structure

CAS No. : 3091068-95-7

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Arf1-GEFs-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Arf1-GEFs-IN-1 相关抗体:
体内研究
(In Vivo)

Arf1-GEFs-IN-1 (Compound 18a) 在小鼠肝脏微粒体 (MLM，半衰期 t1/2 = 31.1 min) 和人类肝脏微粒体 (HLM, t1/2 = 59.2 min) 中的半衰期均较短，并且在小鼠 (94.9%) 和人类 (94.1%) 血浆中的血浆蛋白结合率均较低[1]。
Arf1-GEFs-IN-1 (5 mg/kg, p.o., 持续 2 周) 显著抑制了小鼠 CT26 结肠癌异种移植模型中的肿瘤生长[1]。

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.
分子量

362.45

Formula

C19H18N6S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Arf1-GEFs-IN-1 相关分类

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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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