Pralatrexate
Based on 12 publication(s) in Google Scholar
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate 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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- Pureté : 99.13%
- CAS No.: 146464-95-1
- Formule: C23H23N7O5
- Masse moléculaire:477.47
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-14519
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Publications Citing Use of MedChemExpress (MCE) Pralatrexate
More- Cancer Res. 2025 Nov 21:10.1158/0008-5472.CAN-24-3753. [Abstract]
- Nat Commun. 2026 Oct 1.
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Ocul Surf. 2026 Jul 16:42:129-143.
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Cancers (Basel). 2022 May 20;14(10):2527. [Abstract]
- Antiviral Res. 2024 Jan:221:105787. [Abstract]
- Antimicrob Agents Chemother. 2026 Jul;70(7):e0196025. [Abstract]
- Dis Model Mech. 2023 Mar 1;16(3):dmm049769. [Abstract]
- bioRxiv. 2025 Jun 04.
- bioRxiv. 2024 October 25.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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RT-PCR
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RT-PCR
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RT-PCR
Activité biologique
Description
IC50 & Target
Ki: 13.4 pM (Dihydrofolate reductasean (DHFR))[4]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB | IC50 |
0.47 nM
Compound: PDX, pralatrexate
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Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay
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[PMID: 24111942] |
| KB | IC50 |
0.47 nM
Compound: PTX
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Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
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[PMID: 29425443] |
| KB | IC50 |
1.94 nM
Compound: PDX, pralatrexate
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Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid
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[PMID: 24111942] |
| KB | IC50 |
1.94 nM
Compound: PTX
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Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay
Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay
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[PMID: 29425443] |
| R2 | IC50 |
57 nM
Compound: PDX, pralatrexate
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Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay
Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay
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[PMID: 24111942] |
| R2 | IC50 |
819 nM
Compound: PTX
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Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
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[PMID: 29425443] |
In Vitro
Pralatrexate (100 pM-200 μM; 48-72 hours; T-lymphoma cell lines) treatment exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. The IC50 values at 48 and 72 hours, respectively, are as follows: H9 cells, 1.1 nM and 2.5 nM; P12 cells, 1.7 nM and 2.4 nM; CEM cells, 3.2 nM and 4.2 nM; PF-382 cells, 5.5 nM and 2.7 nM; KOPT-K1 cells, 1 nM and 1.7 nM; DND-41 cells, 97.4 nM and 1.2 nM; and HPB-ALL cells, 247.8 nM and 0.77 nM. HH cells are relatively resistant after 48 hours of exposure, with the IC50 at 72 hours being 2.8 nM[1].
Pralatrexate (2-5.5 nM; 48-72 hours; H9, HH, P12 and PF382 cells) treatment induces potent apoptosis, and caspase-8 and caspase-9 activation[1].
Pralatrexate (3 nM; 16-48 hours; H9 and P12 cells) treatment clearly increases p27 levels and increases the accumulation of educed folate carrier type 1 (RFC-1) in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T-lymphoma cell lines
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Concentration:100 pM-200 µM
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Incubation Time:48 hours, 72 hours
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Result:Exhibited concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines.
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Cell Line:H9, HH, P12 and PF382 cells
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Concentration:2 nM, 3 nM, 4 nM, 5.5 nM
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Incubation Time:48 hours, 72 hours
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Result:Induced potent apoptosis and caspase activation.
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Cell Line:H9 and P12 cells
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Concentration:3 nM
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Incubation Time:16 hours, 24 hours, 48 hours
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Result:Clearly increased p27 levels and increased the accumulation of RFC-1 in cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID-beige mice (5-7-week-old) injected with HH cells[1]
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Dosage:15 mg/kg
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Administration:Intraperitoneal injection; on days 1, 4, 8, and 11
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Result:Showed superior efficacy in T-cell malignancies.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 146464-95-1
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Appearance Solid
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Masse moléculaire 477.47
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Formule C23H23N7O5
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Color Light yellow to yellow
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SMILES
O=C(CC[C@H](NC(C1=CC=C(C=C1)C(CC#C)CC2=NC3=C(N=C(N=C3N=C2)N)N)=O)C(O)=O)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Res
Single-Cell Lineage Tracing Uncovers Resistance Signatures and Sensitizing Strategies to FLT3 Inhibitors in Acute Myeloid Leukemia. [Abstract]2025 Nov 21:10.1158/0008-5472.CAN-24-3753. PMID: 41270153 -
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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 -
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Cancers (Basel)
2022 May 20;14(10):2527. PMID: 35626133 -
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
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 0-1000 nM; 24 h) showed no cytotoxicity for Hala cells.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 20 nM) decreased VSV-G protein expression in VSV-infected (MOI =1) HeLa cells.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 20 nM) decreased the expression of VSV-G mRNA in VSV-infected (MOI =1) HeLa cells.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 0-1000 nM; 24 h) decreased the VSV-G mRNA and protein expression in VSV-infected (MOI =1) HeLa cells.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 0-1000 nM; 72 h) decreased the ORF61 mRNA expression in VSV-infected (MOI =1) ARPE-19 cells.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 2 mg/kg; ip; on days 2, 3, and 4) alleviated peribronchiolar inflammation, decreased interstitial infiltration, and improved alveolar structure in lung tissues; improved ballooning degeneration of hepatocytes and scattered necrosis in liver tissues; PDX not only visibly restored the numberof lymphocytes in the red pulp, but also reduced megakaryocyte infiltration in the spleen tissues; PDX reduced the congestion in capsular space and glomerular hypercellularity in kidney tissues; PDX restored the integrity of intestinal mucosa, and lessen the inflammatory infiltration in intrinsic layer in the intestinal tissuesin VSV-infected ICR mouse model.
Pralatrexate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2024 Jan:221:105787. [Abstract]
Pralatrexate (PDX; 2 mg/kg; ip; on days 2, 3, and 4) decreased the mRNA expression of IL-1α, IL-1β, IL-6, and RANTES in the blood of the VSV-infected ICR mouse model.
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Antimicrob Agents Chemother
Pralatrexate is a potent pan-serotype human adenovirus inhibitor through suppression of dihydrofolate reductase. [Abstract]2026 Jul;70(7):e0196025. PMID: 42206914 -
Dis Model Mech
A Drosophila chemical screen reveals targeting MEK and DGKa mitigates Ras-driven polarity-impaired tumour growth. [Abstract]2023 Mar 1;16(3):dmm049769. PMID: 36861754 -
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Solvant et solubilité
In Vitro:
DMSO : ≥ 50 mg/mL (104.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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 (5.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Enrica Marchi, et al. Pralatrexate Is Synergistic With the Proteasome Inhibitor Bortezomib in in Vitro and in Vivo Models of T-cell Lymphoid Malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58. [Content Brief]
[2]. Francine Foss, et al. Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study. Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. [Content Brief]
[3]. Karen Kelly, et al. Randomized Phase 2b Study of Pralatrexate Versus Erlotinib in Patients With Stage IIIB/IV Non-Small-Cell Lung Cancer (NSCLC) After Failure of Prior Platinum-Based Therapy. J Thorac Oncol. 2012 Jun;7(6):1041-8. [Content Brief]
[4]. F M Sirotnak, et al. A New Analogue of 10-deazaaminopterin With Markedly Enhanced Curative Effects Against Human Tumor Xenografts in Mice. Cancer Chemother Pharmacol. 1998;42(4):313-8. [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 | 2.0944 mL | 10.4719 mL | 20.9437 mL | 52.3593 mL |
| 5 mM | 0.4189 mL | 2.0944 mL | 4.1887 mL | 10.4719 mL | |
| 10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.2359 mL | |
| 15 mM | 0.1396 mL | 0.6981 mL | 1.3962 mL | 3.4906 mL | |
| 20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.6180 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8377 mL | 2.0944 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6981 mL | 1.7453 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3090 mL | |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6545 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2094 mL | 0.5236 mL |
Pralatrexate Related Classifications
HY-10446 Related Classifications
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