Cat. No.: HY-10446

Pralatrexate

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i 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

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pralatrexate Chemical Structure

CAS No.: 146464-95-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i 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^[1]^[2]^[3]^[4]. 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.

IC₅₀ & Target

Ki: 13.4 pM (Dihydrofolate reductasean (DHFR))^[4]

Cellular Effect

Cell Line	Type	Value	Description	References
KB	IC₅₀	0.47 nM Compound: PDX, pralatrexate	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	[PMID: 24111942]
KB	IC₅₀	0.47 nM Compound: PTX	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	[PMID: 29425443]
KB	IC₅₀	1.94 nM Compound: PDX, pralatrexate	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	[PMID: 24111942]
KB	IC₅₀	1.94 nM Compound: PTX	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	[PMID: 29425443]
R2	IC₅₀	57 nM Compound: PDX, pralatrexate	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	[PMID: 24111942]
R2	IC₅₀	819 nM Compound: PTX	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	[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.

Cell Cytotoxicity Assay^[1]

Cell Line:

T-lymphoma cell lines
Concentration:

100 pM-200 µM
Incubation Time:

48 hours, 72 hours
Result:

Exhibited concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines.

Apoptosis Analysis^[1]

Cell Line:

H9, HH, P12 and PF382 cells
Concentration:

2 nM, 3 nM, 4 nM, 5.5 nM
Incubation Time:

48 hours, 72 hours
Result:

Induced potent apoptosis and caspase activation.

Western Blot Analysis^[1]

Cell Line:

H9 and P12 cells
Concentration:

3 nM
Incubation Time:

16 hours, 24 hours, 48 hours
Result:

Clearly increased p27 levels and increased the accumulation of RFC-1 in cells.

In Vivo

The addition of Pralatrexate (15 mg/kg; intraperitoneal injection; on days 1, 4, 8, and 11; SCID-beige mice) to Bortezomib (0.5 mg/kg) enhanced efficacy compared with either drug alone^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID-beige mice (5-7-week-old) injected with HH cells^[1]
Dosage:

15 mg/kg
Administration:

Intraperitoneal injection; on days 1, 4, 8, and 11
Result:

Showed superior efficacy in T-cell malignancies.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 146464-95-1
Appearance Solid
Masse moléculaire 477.47
Formule C₂₃H₂₃N₇O₅
Color Light yellow to yellow
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

All Cell Proliferation/Viability AssayWBRT-PCRHistological Imaging/Staining

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Journal Impact Factor

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
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
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
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Cancers (Basel)

A Drug Screening Revealed Novel Potential Agents against Malignant Pleural Mesothelioma. [Abstract]

2022 May 20;14(10):2527. PMID: 35626133
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
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.
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
bioRxiv

2025 Jun 04.
bioRxiv

2024 October 25.

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0944 mL

10.4719 mL

20.9437 mL

5 mM

0.4189 mL

2.0944 mL

4.1887 mL

10 mM

0.2094 mL

1.0472 mL

2.0944 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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OR (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Pralatrexate

10 Cited Publications

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Pralatrexate

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Publications Citing Use of MedChemExpress (MCE) Pralatrexate

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Pralatrexate Related Classifications

HY-10446 Related Classifications