| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SN-40 targets ASCT2 (human: Ki = 2.42 uM; rat: Ki = 7.29 uM), EAAT1 (Ki = 2.94 uM), EAAT2 (Ki = 5.55 uM), EAAC1/EAAT3 (Ki = 24.43 uM), and EAAT5 (Ki = 5.55 uM). It is a selective AAT inhibitor without significant off-target effects on other transporters.
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|---|---|
| ln Vitro |
In cell-free transporter assays using membrane vesicles or reconstituted proteoliposomes expressing recombinant transporters, SN-40 inhibits Na+-dependent amino acid uptake with Ki values in the low micromolar range. It exhibits competitive inhibition and does not affect transporter protein expression levels.
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| ln Vivo |
In cancer cells, SN-40 (1-50 uM) inhibits glutamine uptake via ASCT2, leading to reduced cell proliferation, induced apoptosis, and decreased activation of mTOR signaling. It shows anti-proliferative effects in various cancer cell lines with dysregulated amino acid metabolism and exhibits synergistic effects with standard chemotherapeutics.
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| Enzyme Assay |
In vitro transporter inhibition assays are performed using membrane vesicles prepared from cells overexpressing recombinant ASCT2 or EAAT transporters. Uptake of 3H-labeled amino acids (e.g., glutamine for ASCT2, glutamate for EAATs) is measured in the presence of varying SN-40 concentrations (0.1-100 uM). Ki values are calculated from Dixon plot analysis of inhibition data.
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| Cell Assay |
Cancer cells (e.g., HCC, breast cancer, glioma) are treated with 1-50 uM SN-40 for 24-72 hours. Amino acid uptake (3H-glutamine) is measured. Cell viability is assessed via MTT or CellTiter-Glo assays. Apoptosis is quantified by flow cytometry (Annexin V/PI). mTOR signaling is assessed by Western blot (p-S6K, p-4EBP1). Synergy studies are performed using combination index analysis.
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| Animal Protocol |
In murine xenograft models of ASCT2-dependent cancers, SN-40 is administered intraperitoneally or orally at 10-50 mg/kg daily for 2-4 weeks. Tumor volume is measured by calipers twice weekly. Plasma and tumor amino acid levels are quantified by LC-MS. Tumor tissue is harvested post-treatment for analysis of proliferation markers (Ki67), apoptosis (TUNEL, caspase-3), and mTOR pathway activation.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies in rodents indicate moderate oral bioavailability (approximately 30-50%) with SN-40. Peak plasma concentrations are reached within 2-4 hours post-oral dosing. The compound shows good tissue distribution, with accumulation in tumor tissues. The elimination half-life ranges from 4-8 hours depending on dose. SN-40 is primarily metabolized by hepatic CYP enzymes.
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| Toxicity/Toxicokinetics |
Toxicity studies in rodents at therapeutic doses (up to 50 mg/kg) show a tolerable safety profile with no significant adverse effects on body weight or major organ function. At higher doses (>100 mg/kg), mild gastrointestinal distress may occur. Standard safety precautions for laboratory chemicals should be followed. SN-40 is for research use only, not for human therapy.
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| References | |
| Additional Infomation |
This is a research-grade inhibitor, not an approved drug. It is used to study the role of amino acid transporters in cancer metabolism and as a tool for developing AAT-targeted anticancer therapies. Molecular formula: C18H20N2O2; molecular weight: 296.36. Purity: ≥98%. Also known as SN40. Protect from light during storage.
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| Molecular Formula |
C18H20N2O2
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|---|---|
| Molecular Weight |
296.363604545593
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| Exact Mass |
296.152
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| CAS # |
2768663-14-3
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| Related CAS # |
SN40 hydrochloride; 2768663-15-4
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| PubChem CID |
164516873
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| Appearance |
White to off-white solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
360
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@@H](CN[C@@H]1C(=O)O)NCC2=CC=C(C=C2)C3=CC=CC=C3
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| InChi Key |
FKDKNHWXEJUEMP-IRXDYDNUSA-N
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| InChi Code |
InChI=1S/C18H20N2O2/c21-18(22)17-10-16(12-20-17)19-11-13-6-8-15(9-7-13)14-4-2-1-3-5-14/h1-9,16-17,19-20H,10-12H2,(H,21,22)/t16-,17-/m0/s1
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| Chemical Name |
(2S,4S)-4-[(4-phenylphenyl)methylamino]pyrrolidine-2-carboxylic acid
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~10 mg/mL (~33.7 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (3.37 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 1 mg/mL (3.37 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 1 mg/mL (3.37 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3743 mL | 16.8714 mL | 33.7427 mL | |
| 5 mM | 0.6749 mL | 3.3743 mL | 6.7485 mL | |
| 10 mM | 0.3374 mL | 1.6871 mL | 3.3743 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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