1. Cell Cycle/DNA Damage
    Apoptosis
  2. Antifolate
    Apoptosis
  3. Pralatrexate

Pralatrexate 

Cat. No.: HY-10446 Purity: 98.13%
Handling Instructions

Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.

For research use only. We do not sell to patients.

Pralatrexate Chemical Structure

Pralatrexate Chemical Structure

CAS No. : 146464-95-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE Pralatrexate

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment[1][2][3][4].

IC50 & Target

Ki: 13.4 pM (Dihydrofolate reductasean (DHFR))[4]

In Vitro

Pralatrexate (100 pM-200 µM; 48-72 hours; T-lymphoma cell lines) treatment exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. The IC50 values at 48 and 72 hours, respectively, are as follows: H9 cells, 1.1 nM and 2.5 nM; P12 cells, 1.7 nM and 2.4 nM; CEM cells, 3.2 nM and 4.2 nM; PF-382 cells, 5.5 nM and 2.7 nM; KOPT-K1 cells, 1 nM and 1.7 nM; DND-41 cells, 97.4 nM and 1.2 nM; and HPB-ALL cells, 247.8 nM and 0.77 nM. HH cells are relatively resistant after 48 hours of exposure, with the IC50 at 72 hours being 2.8 nM[1].
Pralatrexate (2-5.5 nM; 48-72 hours; H9, HH, P12 and PF382 cells) treatment induces potent apoptosis, and caspase-8 and caspase-9 activation[1].
Pralatrexate (3 nM; 16-48 hours; H9 and P12 cells) treatment clearly increases p27 levels and increases the accumulation of educed folate carrier type 1 (RFC-1) in cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: T-lymphoma cell lines
Concentration: 100 pM-200 µM
Incubation Time: 48 hours, 72 hours
Result: Exhibited concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines.

Apoptosis Analysis[1]

Cell Line: H9, HH, P12 and PF382 cells
Concentration: 2 nM, 3 nM, 4 nM, 5.5 nM
Incubation Time: 48 hours, 72 hours
Result: Induced potent apoptosis and caspase activation.

Western Blot Analysis[1]

Cell Line: H9 and P12 cells
Concentration: 3 nM
Incubation Time: 16 hours, 24 hours, 48 hours
Result: Clearly increased p27 levels and increased the accumulation of RFC-1 in cells.
In Vivo

The addition of Pralatrexate (15 mg/kg; intraperitoneal injection; on days 1, 4, 8, and 11; SCID-beige mice) to Bortezomib (0.5 mg/kg) enhanced efficacy compared with either drug alone[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID-beige mice (5-7-week-old) injected with HH cells[1]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; on days 1, 4, 8, and 11
Result: Showed superior efficacy in T-cell malignancies.
Clinical Trial
Molecular Weight

477.47

Formula

C₂₃H₂₃N₇O₅

CAS No.
SMILES

O=C(CC[[email protected]](NC(C1=CC=C(C=C1)C(CC#C)CC2=NC3=C(N=C(N=C3N=C2)N)N)=O)C(O)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (104.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0944 mL 10.4719 mL 20.9437 mL
5 mM 0.4189 mL 2.0944 mL 4.1887 mL
10 mM 0.2094 mL 1.0472 mL 2.0944 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.23%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PralatrexateAntifolateApoptosisdihydrofolatereductasefolylpolyglutamatesynthetasecytotoxicityp27RFC-1antitumorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pralatrexate
Cat. No.:
HY-10446
Quantity:
MCE Japan Authorized Agent: