Name: Pralatrexate
Brand: Selleck Chemicals
SKU: S1497
Availability: InStock
Rating: 5 (18 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.58

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other DHFR Inhibitors	Calcium Folinate Aminopterin Diaveridine

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 28 mg/mL (58.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.400mg/ml (2.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.230mg/ml (0.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 4.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	477.47	Formula	C₂₃H₂₃N₇O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	146464-95-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 754230			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

Mechanism of Action

Targets/IC₅₀/Ki	DHFR
In vitro	Pralatrexate and bortezomib exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. This compound shows synergism when combined with bortezomib in all cell lines studied. It also induces potent apoptosis and caspase activation when combined with bortezomib across the panel. The agent significantly modulates the expression of p27, NOXA, HH3, and RFC-1 as assessed by Western blot assays. This compound is rationally designed for improved cellular transport via RFC-1, and to have greater intracellular drug retention through the enhanced formation of polyglutamylated conjugates. It is thought to exert its pharmacological effect primarily through inhibition of DHFR, having an IC50 in the picomolar range. This chemical demonstrates superior intracellular transport via the reduced folate carrier, and increased accumulation within cells by enhanced polyglutamylation. It exhibits antitumor activity that is superior to the activity of other antifolates. Its 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20501616/ [2] https://pubmed.ncbi.nlm.nih.gov/19221750/ [3] https://pubmed.ncbi.nlm.nih.gov/18600598/ [4] https://pubmed.ncbi.nlm.nih.gov/23881211/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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Frequently Asked Questions

Question 1:
We are just wondering if it is a racemic mixture or a monomer? Will you please let us know?

Answer:
It is the S enantiomer.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Pralatrexate DHFR inhibitor

Chemical Structure

Molecular Weight: 477.47