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Arf1-GEFs-IN-1
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Catalog No. T212402Cas No. 3091068-95-7
Arf1-GEFs-IN-1 is a potent and orally active inhibitor of ADP-ribosylation factor 1-guanine nucleotide exchange factors (Arf1-GEFs), exhibiting an IC50 value of 40 μM in CT26 cells. Primarily, Arf1-GEFs-IN-1 induces tumor regression by triggering anti-tumor immune responses rather than direct cytotoxicity. It effectively enhances CCL5 expression and demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 is applicable in colon cancer research.
Arf1-GEFs-IN-1
Copy Product Info😃Good
Catalog No. T212402Cas No. 3091068-95-7
Arf1-GEFs-IN-1 is a potent and orally active inhibitor of ADP-ribosylation factor 1-guanine nucleotide exchange factors (Arf1-GEFs), exhibiting an IC50 value of 40 μM in CT26 cells. Primarily, Arf1-GEFs-IN-1 induces tumor regression by triggering anti-tumor immune responses rather than direct cytotoxicity. It effectively enhances CCL5 expression and demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 is applicable in colon cancer research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Arf1-GEFs-IN-1 is a potent and orally active inhibitor of ADP-ribosylation factor 1-guanine nucleotide exchange factors (Arf1-GEFs), exhibiting an IC50 value of 40 μM in CT26 cells. Primarily, Arf1-GEFs-IN-1 induces tumor regression by triggering anti-tumor immune responses rather than direct cytotoxicity. It effectively enhances CCL5 expression and demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 is applicable in colon cancer research. |
| In vitro | Arf1-GEFs-IN-1 (Compound 18a) effectively suppresses tumors in CT26 cells with an impressive rate of 80.7% and boasts a significantly improved safety profile, having an IC 50 of 193.6 μM in 3T3 cells. While Arf1-GEFs-IN-1 (2-50 μM) does not directly activate T cells, it influences the immune microenvironment via tumor cells, potentially enhancing tumor immunogenicity through Arf1 inhibition in CT26 cells. |
| In vivo | Arf1-GEFs-IN-1 (Compound 18a) exhibits a short half-life in both mouse liver microsomes (MLM, half-life t1/2 = 31.1 min) and human liver microsomes (HLM, t1/2 = 59.2 min). It also demonstrates a low plasma protein binding rate in mouse (94.9%) and human (94.1%) plasma. Administered orally at 5 mg/kg for two weeks, Arf1-GEFs-IN-1 significantly inhibits tumor growth in a mouse CT26 colon cancer xenograft model. |
| Molecular Weight | 362.45 |
| Formula | C19H18N6S |
| Cas No. | 3091068-95-7 |
| Smiles | N(/N=C/C=1C=C2C(=CC1)NC=C2)C3=C4C5=C(SC4=NC=N3)CN(C)CC5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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