Pralatrexate (NSC 754230)

For research use only.

Catalog No.S1497

10 publications

Pralatrexate (NSC 754230) Chemical Structure

CAS No. 146464-95-1

Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.

Selleck's Pralatrexate (NSC 754230) has been cited by 10 publications

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 (NSC 754230) purchased from Selleck.

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Biological Activity

Description Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
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 M17JfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\EPVYhcA>? MmnyS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gT2Ih[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDSSmMwTlKjbIDoZU9RS0[WIHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkS3JI5O NEXibGEzPDFzMUm0Ni=>
Chinese hamster R2 cells MkjlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzQSppkQTZiaB?= MXrHdo94fGhiaX7obYJqfGmxbjDv[kBEcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeIVzNWKudXWgZZN{[XluIFnDOVA:OC5yNUeg{txO M4DNSlI1OTFzOUSy

... 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]


Solubility (25°C)

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

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Chemical Information

Molecular Weight 477.47


CAS No. 146464-95-1
Storage powder
in solvent
Synonyms N/A
Smiles C#CCC(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02594267 Completed Drug: Pralatrexate Injection Peripheral T-Cell Lymphoma (PTCL) Acrotech Biopharma LLC|Axis Clinicals Limited November 10 2015 Phase 1
NCT01947140 Recruiting Drug: Pralatrexate|Drug: Romidepsin Lymphoid Malignancies|Multiple Myeloma|Lymphoma|Hodgkin Lymphoma|Non-hodgkin Lymphoma Jennifer Amengual|Columbia University September 9 2013 Phase 1|Phase 2
NCT01532011 Completed Drug: Erlotinib|Drug: Pralatrexate Advanced Cancers|Solid Tumors M.D. Anderson Cancer Center March 2012 Phase 1
NCT01420679 Terminated Drug: Pralatrexate Injection Peripheral T-cell Lymphoma Spectrum Pharmaceuticals Inc August 2011 Phase 3

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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