LSN 3213128 |
Katalog-Nr.GC36486
One-Click Copy Product Info
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LSN 3213128 ist ein selektives, nicht-klassisches, oral bioverfÜgbares Antifolat mit starker und spezifischer HemmaktivitÄt fÜr die Aminoimidazol-4-carboxamid-Ribonukleotid-Formyltransferase (AICARFT), mit einem IC50 von 16 nM fÜr die AICARFT-Enzymhemmung und 19 nM in Zellen. Anti-Tumor-AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1941211-99-9
Sample solution is provided at 25 µL, 10mM.
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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 for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity[1]. IC50: 16 nM (AICARFT), 19 nM (AICARFT in cells)[1]
[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.
| Cas No. | 1941211-99-9 | SDF | |
| Canonical SMILES | O=C1NC=CC2=C1C=C(NS(=O)(C3=CC=C(N4CC[C@@H](O)C4)S3)=O)C(F)=C2 | ||
| Formula | C17H16FN3O4S2 | M.Wt | 409.46 |
| Löslichkeit | DMSO: 62.5 mg/mL (152.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4422 mL | 12.2112 mL | 24.4224 mL |
| 5 mM | 488.4 μL | 2.4422 mL | 4.8845 mL |
| 10 mM | 244.2 μL | 1.2211 mL | 2.4422 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)