Plevitrexed
Based on 1 Customer Validation
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical. Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Reinheit: 99.35%
- CAS. Nr.: 153537-73-6
- Formel: C26H25FN8O4
- Molecular Weight:532.53
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | IC50 |
0.024 μM
Compound: 35
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Growth inhibition of murine tumor L1210 cell line
Growth inhibition of murine tumor L1210 cell line
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[PMID: 10508430] |
| L1210 | IC50 |
1.4 nM
Compound: 35
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Inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
Inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
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[PMID: 10508430] |
| L1210 (1565) | IC50 |
1.3 μM
Compound: 35
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Inhibition of cell growth in culture against murine tumor L1210:1565 cell lines
Inhibition of cell growth in culture against murine tumor L1210:1565 cell lines
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[PMID: 10508430] |
| L1210 (RD1694) | IC50 |
0.076 μM
Compound: 35
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Tested for inhibition of cell growth in culture against murine tumor L1210:RD1694 cell lines
Tested for inhibition of cell growth in culture against murine tumor L1210:RD1694 cell lines
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[PMID: 10508430] |
ZD9331 inhibits the transport of [3H]-methotrexate into L1210 and W1L2 cells with a Ki of∼1 µM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 153537-73-6
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Appearance Solid
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Molecular Weight 532.53
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Formel C26H25FN8O4
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Color White to light yellow
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SMILES
O=C(NC(C)=N1)C2=C1C=C(C)C(CN(C3=CC=C(C(N[C@H](C(O)=O)CCC4=NNN=N4)=O)C(F)=C3)CC#C)=C2
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Synonyms
ZD 9331; BGC9331
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (187.78 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 2.5 mg/mL (4.69 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Reinheit & Dokumentation
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Data Sheet (272 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)
Verweise
[1]. Tochowicz A, et al. Development and binding mode assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-D-glutamic acid (BGC 945), a novel thymidylate synthase inhibitor that targets tumor cells. J Med Chem. 2013 Jul 11;56(13):5446-55. [Content Brief]
[3]. Marsham PR, et al. Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors. J Med Chem. 1999 Sep 23;42(19):3809-20. [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. 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 |
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| DMSO | 1 mM | 1.8778 mL | 9.3891 mL | 18.7783 mL | 46.9457 mL |
| 5 mM | 0.3756 mL | 1.8778 mL | 3.7557 mL | 9.3891 mL | |
| 10 mM | 0.1878 mL | 0.9389 mL | 1.8778 mL | 4.6946 mL | |
| 15 mM | 0.1252 mL | 0.6259 mL | 1.2519 mL | 3.1297 mL | |
| 20 mM | 0.0939 mL | 0.4695 mL | 0.9389 mL | 2.3473 mL | |
| 25 mM | 0.0751 mL | 0.3756 mL | 0.7511 mL | 1.8778 mL | |
| 30 mM | 0.0626 mL | 0.3130 mL | 0.6259 mL | 1.5649 mL | |
| 40 mM | 0.0469 mL | 0.2347 mL | 0.4695 mL | 1.1736 mL | |
| 50 mM | 0.0376 mL | 0.1878 mL | 0.3756 mL | 0.9389 mL | |
| 60 mM | 0.0313 mL | 0.1565 mL | 0.3130 mL | 0.7824 mL | |
| 80 mM | 0.0235 mL | 0.1174 mL | 0.2347 mL | 0.5868 mL | |
| 100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4695 mL |
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