Nolatrexed dihydrochloride
Based on 2 publication(s) in Google Scholar
Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.
For research use only. We do not sell to patients.
- Purity: 98.47%
- CAS No.: 152946-68-4
- Formula: C14H14Cl2N4OS
- Molecular Weight:357.26
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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) Nolatrexed dihydrochloride
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Biological Activity
Ki: 11 nM (Human Thymidylate Synthase)[1]
Nolatrexed (6-h exposure) dihydrochloride shows a certain inhibitory effect on CCRF-CEM cells in intermittent exposure[2].
Nolatrexed (1 nM-1.2 mM, 10 days) dihydrochloride significantly increases sulfotransferases expressions in HepG2 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nolatrexed dihydrochloride (50 mg/kg, i.v.) shows half-life, AUC, distribution factor and plasma clearance (CL) of 3.020 h, 89.972 mg/L/h, 0.831 L/kg, and 0.556 L/h/kg, respectively, in mice[4].
Nolatrexed dihydrochloride (200 mg/kg, p.o.) shows half-life, AUC, peak time (T(max)) and peak concentration (C(max)) for orally administered drug of 5.046 h, 84.893 mg/L/h, 1.000 h, and 18.0 mg/L, respectively, in mice[4].
Nolatrexed dihydrochloride (60 mg/m2; i.p.; every 4 h; 5 d) results in significant tumor growth retardation in nude mice bearing the HeLa Bu25TK- human cervical cell line[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 152946-68-4
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Appearance Solid
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Molecular Weight 357.26
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Formula C14H14Cl2N4OS
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Color Light yellow to yellow
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SMILES
[H]Cl.O=C1N=C(N)NC2=C1C(SC3=CC=NC=C3)=C(C)C=C2.[H]Cl
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Synonyms
AG 337
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Commun Biol
Serine hydroxymethyltransferase as a potential target of antibacterial agents acting synergistically with one-carbon metabolism-related inhibitors. [Abstract]2022 Jun 23;5(1):619. PMID: 35739195
Solvent & Solubility
DMSO : 50 mg/mL (139.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (139.95 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (5.82 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 (5.82 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 25 mg/mL (69.98 mM); Clear solution; Need ultrasonic and warming
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37(6):509-17. [Content Brief]
[2]. McGuire JJ, et al. Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines. [Content Brief]
[3]. Maiti S, et al. Regulations of expressions of rat/human sulfotransferases by anticancer drug, nolatrexed, and micronutrients. Anticancer Drugs. 2022 Jan 1;33(1):e525-e533. [Content Brief]
[5]. Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37(6):509-17. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.7991 mL | 13.9954 mL | 27.9908 mL | 69.9770 mL |
| 5 mM | 0.5598 mL | 2.7991 mL | 5.5982 mL | 13.9954 mL | |
| 10 mM | 0.2799 mL | 1.3995 mL | 2.7991 mL | 6.9977 mL | |
| 15 mM | 0.1866 mL | 0.9330 mL | 1.8661 mL | 4.6651 mL | |
| 20 mM | 0.1400 mL | 0.6998 mL | 1.3995 mL | 3.4989 mL | |
| 25 mM | 0.1120 mL | 0.5598 mL | 1.1196 mL | 2.7991 mL | |
| 30 mM | 0.0933 mL | 0.4665 mL | 0.9330 mL | 2.3326 mL | |
| 40 mM | 0.0700 mL | 0.3499 mL | 0.6998 mL | 1.7494 mL | |
| 50 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3995 mL | |
| 60 mM | 0.0467 mL | 0.2333 mL | 0.4665 mL | 1.1663 mL | |
| 80 mM | 0.0350 mL | 0.1749 mL | 0.3499 mL | 0.8747 mL | |
| 100 mM | 0.0280 mL | 0.1400 mL | 0.2799 mL | 0.6998 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Nolatrexed dihydrochloride Related Classifications
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