LSN 3213128
Based on 2 publication(s) in Google Scholar
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT) with IC50 of 16 nM. LSN 3213128 exhibits anti-tumor activity.
For research use only. We do not sell to patients.
- Purity: 98.36%
- CAS No.: 1941211-99-9
- Formula: C17H16FN3O4S2
- Molecular Weight:409.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LSN 3213128
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Biological Activity
IC50: 16 nM (AICARFT)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | GI50 |
44 nM
Compound: 28a
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Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition using regular folate media after 7 days by Alamar blue assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition using regular folate media after 7 days by Alamar blue assay
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[PMID: 29072452] |
| NCI-H460 | GI50 |
25 nM
Compound: 28a
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Cytotoxicity against human NCI-H460 cells assessed as growth inhibition using low folate media after 7 days by Alamar blue assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition using low folate media after 7 days by Alamar blue assay
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[PMID: 29072452] |
| NCI-H460 | GI50 |
6580 nM
Compound: 28a
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Cytotoxicity against human NCI-H460 cells assessed as growth inhibition using regular folate media after 7 days by Alamar blue assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition using regular folate media after 7 days by Alamar blue assay
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[PMID: 29072452] |
LSN 3213128 inhibits the proliferation of cancer cells NCI-H460 and MDA-MB-231 with GI50s of 3470 nM and 44 nM (in standard RPMI medium). LSN 3213128 causes the accumulation of 5-aminoimidazole-4-carboxamide ribonucleotide (ZMP) in NCI-H460, EC50s in low-folate medium and standard RPMI medium are 8 nM and 356 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MDA-MB-231met2 xenograft models[1]
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Dosage:30-60 mg/kg
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Administration:po, twice daily for 22 days
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Result:Inhibited the tumor growth.
Chemical Information
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CAS No. 1941211-99-9
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Appearance Solid
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Molecular Weight 409.46
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Formula C17H16FN3O4S2
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Color Off-white to pink
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SMILES
O=C1NC=CC2=C1C=C(NS(=O)(C3=CC=C(N4CC[C@@H](O)C4)S3)=O)C(F)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Antiviral Res
Pralatrexate inhibited the replication of varicella zoster virus and vesicular stomatitis virus: An old dog with new tricks. [Abstract]2024 Jan:221:105787. PMID: 38145756
Solvent & Solubility
DMSO : 83.33 mg/mL (203.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Fales KR, et al. Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model. J Med Chem. 2017 Dec 14;60(23):9599-9616. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4422 mL | 12.2112 mL | 24.4224 mL | 61.0560 mL |
| 5 mM | 0.4884 mL | 2.4422 mL | 4.8845 mL | 12.2112 mL | |
| 10 mM | 0.2442 mL | 1.2211 mL | 2.4422 mL | 6.1056 mL | |
| 15 mM | 0.1628 mL | 0.8141 mL | 1.6282 mL | 4.0704 mL | |
| 20 mM | 0.1221 mL | 0.6106 mL | 1.2211 mL | 3.0528 mL | |
| 25 mM | 0.0977 mL | 0.4884 mL | 0.9769 mL | 2.4422 mL | |
| 30 mM | 0.0814 mL | 0.4070 mL | 0.8141 mL | 2.0352 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5264 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2211 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0176 mL | |
| 80 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7632 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6106 mL |
LSN 3213128 Related Classifications
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