Pralatrexate

Catalog No.S1497

Pralatrexate  Chemical Structure

Molecular Weight(MW): 477.47

Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock
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Cited by 1 Publication

1 Customer Review

  • PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).

    Blood, 2018, 131(4):397-407. Pralatrexate purchased from Selleck.

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Biological Activity

Description Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.
Targets
DHFR [1]
In vitro

Pralatrexate and bortezomib exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. Pralatrexate shows synergism when combined with bortezomib in all cell lines studied. Pralatrexate also induces potent apoptosis and caspase activation when combined with bortezomib across the panel. Pralatrexate significantly modulates the expression of p27, NOXA, HH3, and RFC-1 as assessed by Western blot assays. [1] Pralatrexate is rationally designed for improved cellular transport via RFC-1, and to have greater intracellular drug retention through the enhanced formation of polyglutamylated conjugates. Pralatrexate is thought to exert its pharmacological effect primarily through inhibition of DHFR, having an IC50 in the picomolar range. [2] Pralatrexate demonstrates superior intracellular transport via the reduced folate carrier, and increased accumulation within cells by enhanced polyglutamylation. Pralatrexate exhibits antitumor activity that is superior to the activity of other antifolates. [3] Pralatrexate's enhanced activity relative to methotrexate (MTX) is due to its much more rapid rate of transport and polyglutamation, the former less important when the carrier is saturated. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human KB cells NVXjSHNvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3Tqclk3KGh? NHjhUI9Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBMSiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJHJHSy:IUnHsdIhiN1CFRmSgZYZ1\XJiOU[gbJJ{KGK7IFPlcIxVcXSncj3icJVmKGG|c3H5MEBKSzVyPUCuOFchdk1? M3\ZW|I1OTFzOUSy
Chinese hamster R2 cells NGXlbIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LGfFk3KGh? NVLhUW5YT3Kxd4ToJIlvcGmkaYTpc44hd2ZiQ3jpcoV{\SCqYX3zeIVzKFJ{IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWEOIVESgZYZ1\XJiOU[gbJJ{KGK7IFPlcIxVcXSncj3icJVmKGG|c3H5MEBKSzVyPUCuNFU4KM7:TR?= NVfvc3FDOjRzMUG5OFI>

... Click to View More Cell Line Experimental Data

In vivo Pralatrexate treatment results in treatment-related toxicity in MV522 mice models, as determined by significant weight loss in some animals prior to death; however, remaining mice regains all lost weight by Day 35. [2]

Protocol

Solubility (25°C)

In vitro DMSO 28 mg/mL (58.64 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 477.47
Formula

C23H23N7O5

CAS No. 146464-95-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03598998 Recruiting Recurrent Mature T- and NK-Cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides|Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Refractory Mycosis Fungoides City of Hope Medical Center|National Cancer Institute (NCI) February 4 2019 Phase 1|Phase 2
NCT03598998 Recruiting Recurrent Mature T- and NK-Cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides|Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Refractory Mycosis Fungoides City of Hope Medical Center|National Cancer Institute (NCI) February 4 2019 Phase 1|Phase 2
NCT03355768 Withdrawn Lymphoma T-Cell Peripheral Jennifer Amengual|Columbia University September 1 2018 Phase 3
NCT03355768 Withdrawn Lymphoma T-Cell Peripheral Jennifer Amengual|Columbia University September 1 2018 Phase 3
NCT03240211 Recruiting PTCL|CTCL Owen A. O''Connor|University of Bologna|Samsung Medical Center|Merck Sharp & Dohme Corp.|Columbia University June 1 2018 Phase 1
NCT03161223 Recruiting Lymphoma T-Cell Columbia University|University of Bologna|Samsung Medical Center|Celgene June 1 2018 Phase 1|Phase 2

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Frequently Asked Questions

  • Question 1:

    We are just wondering if S1497 a racemic mixture or a monomer? Will you please let us know?

  • Answer:

    S1497 Pralatrexate is S enantiomer.

DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID