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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
😃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]
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals 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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