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| Targets |
ARI-3144 targets fibroblast activation protein (FAP), a serine protease that is highly expressed in the stroma of many solid tumors but is largely absent from normal adult tissues. FAP cleaves ARI-3144 to release a potent proteasome inhibitor. This released inhibitor then targets the proteasome, a key component of the ubiquitin-proteasome system, leading to the disruption of protein homeostasis and cell death in cancer cells.
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| ln Vitro |
In vitro, ARI-3144 acts as an excellent substrate for FAP. Its activation by FAP leads to the inhibition of the proteasome. Its activity is characterized by its ability to be selectively cleaved by FAP, which can be measured in enzyme assays using recombinant FAP. Specific IC50 values for proteasome inhibition are not detailed in the available literature.
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| ln Vivo |
In vivo, ARI-3144 is designed for solid tumor research. As a FAP-activated prodrug, it is expected to show antitumor activity in FAP-positive tumor models. Specific animal model data are not available in the provided literature.
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| Enzyme Assay |
In vitro enzyme assay protocols for ARI-3144 typically involve measuring its cleavage by fibroblast activation protein (FAP). Recombinant FAP is incubated with ARI-3144, and the release of the proteasome inhibitor moiety is monitored by HPLC or mass spectrometry. Proteasome inhibition activity can be assessed using fluorogenic substrates in the presence of the activated compound.
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| Cell Assay |
In vitro cell-based assay protocols for ARI-3144 involve treating FAP-expressing cancer cells or co-cultures of cancer cells and FAP-positive fibroblasts with the compound. Cell viability, proliferation, and apoptosis are measured to assess its antitumor activity. The selectivity of the prodrug can be demonstrated by comparing its effects on FAP-positive versus FAP-negative cells.
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| Animal Protocol |
In vivo animal experimental protocols for ARI-3144 would typically involve using mouse xenograft models of solid tumors, particularly those with high FAP expression in the stroma. The compound is administered systemically, and tumor growth inhibition, biomarker changes, and survival are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ARI-3144 have not been characterized in published studies. Its molecular weight is 498.53. As a prodrug, its activation by FAP in the tumor microenvironment would influence its local and systemic pharmacokinetics. Specific parameters such as half-life and bioavailability have not been reported.
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| Toxicity/Toxicokinetics |
Toxicological data for ARI-3144 are limited. As a FAP-activated prodrug, it is expected to have an improved safety profile compared to systemic proteasome inhibitors by restricting the active drug's release to the tumor site. It is intended for research use only.
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| References | |
| Additional Infomation |
ARI-3144 is a research-grade compound used as a FAP-activated proteasome inhibitor for solid tumor research. Its design is based on a tumor-selective prodrug strategy. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves FAP-mediated activation to release a proteasome inhibitor. The compound is available exclusively for research purposes.
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| Molecular Formula |
C28H26N4O5
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|---|---|
| Molecular Weight |
498.53
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| CAS # |
1426305-25-0
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| Appearance |
White to off-white solid powder
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| Density |
1.369±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
862.820±65.00 °C(Press: 760.00 Torr)(predicted)
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| LogP |
0
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~200.59 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0059 mL | 10.0295 mL | 20.0590 mL | |
| 5 mM | 0.4012 mL | 2.0059 mL | 4.0118 mL | |
| 10 mM | 0.2006 mL | 1.0029 mL | 2.0059 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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