| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target of AMPC is trefoil factor 3 (TFF3), a protein involved in cell proliferation and survival. AMPC specifically binds to Cys57 of TFF3. By monomerizing dimeric TFF3, it inhibits the oncogenic functions of TFF3, which are implicated in colorectal cancer and other malignancies.
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| ln Vitro |
In CMS4 CRC cells, AMPC inhibits cell growth; in SW620 (high TFF3 expression), Caco-2, and SW480 (low TFF3 expression) cells, the IC50 values are 2.63 μM, 4.65 μM, and 69.69 μM, respectively[1]. In SW620 and Caco2 cells, 1-10 μM dramatically lowers the overall cellular levels of TFF3 in a dose-dependent manner[1]. By inhibiting TFF3, AMPC causes apoptosis in a dose-dependent manner. In comparison to control cells, it also causes a decrease in the S-phase population and an increase in caspase 3/7 activity[1].
In vitro, AMPC inhibits cell proliferation, survival, and CSC-like behavior in TFF3-positive CMS4 colorectal cancer cells. It is a potent inhibitor of TFF3 function. It also exhibits antibacterial properties against pathogens such as Escherichia coli. |
| ln Vivo |
When mice are treated with AMPC (intraperitoneal injection; 40 mg/kg; once daily), their tumor volume significantly decreases in comparison to mice treated with saline starting on day 11. In SW620 tumors, AMPC causes greater regions of tumor necrosis and an increase in the area of cells exhibiting apoptotic characteristics. In vivo, AMPC also dramatically lowers serum and tumor TFF3 levels.
In vivo, AMPC has shown antitumor activity in preclinical models of colorectal cancer. It can be used alone or in combination with 5-fluorouracil (5-FU) for cancer research. Its efficacy in vivo supports its potential as a therapeutic agent. |
| Enzyme Assay |
Non-cellular assays for AMPC typically involve measuring its binding to TFF3 using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Its ability to monomerize dimeric TFF3 can be assessed using size-exclusion chromatography or cross-linking assays.
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| Cell Assay |
Cellular assays for AMPC are conducted using TFF3-positive colorectal cancer cell lines. Cells are treated with the compound, and cell proliferation, survival, and CSC-like behavior are assessed using MTT assays, colony formation assays, and flow cytometry for CSC markers.
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| Animal Protocol |
Animal/Disease Models: SW620 cells are subcutaneously (sc) injected into nude mice[1]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; 40 mg/kg; one time/day Experimental Results: Lead to tumor decrease in vivo. Results in a marked reduction of Ki67 expression in tumor. In vivo animal experiments for AMPC typically use mouse xenograft models of colorectal cancer. The compound is administered orally or via injection, and tumor growth inhibition is measured. Its effects on TFF3 signaling and CSC populations are assessed in tumor tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of AMPC are not extensively detailed. As a small molecule, its bioavailability and half-life would depend on its formulation and route of administration. Further studies are needed to characterize its ADME properties.
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| Toxicity/Toxicokinetics |
Toxicological data for AMPC are limited, as it is a research compound. It is for research use only and not for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Ru-Mei Chen, et al. Pharmacological Inhibition of TFF3 Enhances Sensitivity of CMS4 Colorectal Carcinoma to 5-Fluorouracil through Inhibition of p44/42 MAPK. Int J Mol Sci. 2019 Dec 9;20(24):6215
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| Additional Infomation |
AMPC is a first-in-class TFF3 inhibitor with potential as an anticancer agent. It is a valuable research tool for studying the role of TFF3 in cancer biology and for validating TFF3 as a therapeutic target. It is being investigated for the treatment of colorectal cancer and other TFF3-driven malignancies.
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| Molecular Formula |
C25H16FN3O3
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|---|---|
| Molecular Weight |
425.411249160767
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| Exact Mass |
425.117
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| CAS # |
2254434-33-6
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| PubChem CID |
142491885
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
32
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| Complexity |
882
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CN=C1F)C2=CC=C(C=C2)C3C(=C(OC4=C3C(=O)OC5=CC=CC=C54)N)C#N
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| InChi Key |
QYTOMCGQPLOOOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H16FN3O3/c1-13-10-16(12-29-23(13)26)14-6-8-15(9-7-14)20-18(11-27)24(28)32-22-17-4-2-3-5-19(17)31-25(30)21(20)22/h2-10,12,20H,28H2,1H3
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| Chemical Name |
2-amino-4-[4-(6-fluoro-5-methylpyridin-3-yl)phenyl]-5-oxo-4H-pyrano[3,2-c]chromene-3-carbonitrile
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 115 mg/mL (270.33 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6 mg/mL (14.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3507 mL | 11.7534 mL | 23.5067 mL | |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 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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