Home Tools
Log in
Cart

Pralatrexate

Catalog No. T6120   CAS 146464-95-1
Synonyms: Folotyn, 10-Propargyl-10-deazaaminopterin

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

All TargetMol products are for research or drug registration purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose in violation of laws and regulations.
Pralatrexate Chemical Structure
Pralatrexate, CAS 146464-95-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 44.00
5 mg In stock $ 68.00
10 mg In stock $ 117.00
25 mg In stock $ 172.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 98.56%
Purity: 98.12%
Purity: 94.32%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.
Targets&IC50 Axl (SUM149 cells):0.43 μM, Axl (KPL-4 cells):0.16 μM
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 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]
Synonyms Folotyn, 10-Propargyl-10-deazaaminopterin
Molecular Weight 477.47
Formula C23H23N7O5
CAS No. 146464-95-1

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27 mg/mL (56.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Marchi E, et al. Clin Cancer Res, 2010, 16(14), 3648-3658. 2. Izbicka E, et al. Cancer Chemother Pharmacol, 2009, 64(5), 993-999. 3. Molina JR, et al. IDrugs, 2008, 11(7), 508-521. 4. Visentin M, et al. Cancer Chemother Pharmacol, 2013, 72(3), 597-606.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library EMA Approved Drug Library FDA-Approved Kinase Inhibitor Library Inhibitor Library

Related Products

Related compounds with same targets
Dihydrokaempferol 5-LOX-IN-2 BAY 11-7082 Indirubin Vistusertib CGP 3466B maleate Pilaralisib analogue SACLAC

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pralatrexate 146464-95-1 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Tyrosine Kinase/Adaptors Antifolate TAM Receptor DHFR antitumor folylpolyglutamate Folotyn cytotoxicity inhibit Inhibitor RFC-1 dihydrofolate p27 reductase synthetase 10-Propargyl-10-deazaaminopterin inhibitor

 

TargetMol