Home Metabolism DHFR inhibitor - Apoptosis related activator Pralatrexate For research use only.

Pralatrexate

Synonyms: NSC 754230

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

Pralatrexate Chemical Structure

Pralatrexate Chemical Structure

CAS: 146464-95-1

Selleck's Pralatrexate has been cited by 15 Publications

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Purity & Quality Control

Batch: S149701 DMSO] 28 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.58%
99.58

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human KB cells Growth inhibition assay 96 h Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay, IC50=0.47 nM 24111942
Chinese hamster R2 cells Growth inhibition assay 96 h Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay, IC50=0.057 μM 24111942
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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. Pralatrexate induces tumor cell apoptosis.
Targets
DHFR [1]
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02594267 Completed Peripheral T-Cell Lymphoma (PTCL) Acrotech Biopharma Inc.|Axis Clinicals Limited November 10 2015 Phase 1
NCT01947140 Completed Lymphoid Malignancies|Multiple Myeloma|Lymphoma|Hodgkin Lymphoma|Non-hodgkin Lymphoma Jennifer Amengual|Columbia University September 9 2013 Phase 1|Phase 2
NCT01532011 Completed Advanced Cancers|Solid Tumors M.D. Anderson Cancer Center March 2012 Phase 1
NCT01114282 Completed Multiple Myeloma Stanford University|National Comprehensive Cancer Network August 2010 Phase 1

Chemical lnformation & Solubility

Molecular Weight 477.47 Formula

C23H23N7O5
CAS No. 146464-95-1 SDF Download Pralatrexate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 28 mg/mL ( (58.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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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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