Pralatrexate (NSC 754230)

Catalog No.S1497

For research use only.

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.

Pralatrexate (NSC 754230) Chemical Structure

CAS No. 146464-95-1

Selleck's Pralatrexate (NSC 754230) has been cited by 13 publications

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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.
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 MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPxPVYhcA>? MY\Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDLRkBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIGLGR{9HWmGucHjhM3BETlRiYX\0[ZIhQTZiaILzJIJ6KEOnbHzUbZRmei2kbIXlJIF{e2G7LDDJR|UxRTBwNEegcm0> NV7lNoNHOjRzMUG5OFI>
Chinese hamster R2 cells NYnu[3BXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1XTVlk3KGh? NH3NPHdIem:5dHigbY5pcWKrdHnvckBw\iCFaHnu[ZNmKGijbYP0[ZIhWjJiY3XscJMh\XiycnXzd4lv\yCqdX3hckBRS0[WNDDh[pRmeiB7NjDodpMh[nliQ3XscHRqfGW{LXLseYUh[XO|YYmsJGlEPTB;MD6wOVch|ryP NXO1N2h7OjRzMUG5OFI>
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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 477.47
Formula

C23H23N7O5

CAS No. 146464-95-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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
NCT01114282 Completed Drug: velcade|Drug: Pralatrexate Multiple Myeloma Stanford University|National Comprehensive Cancer Network August 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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