Pralatrexate

Catalog No.S1497

Pralatrexate  Chemical Structure

Molecular Weight(MW): 477.47

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

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock
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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.
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 Mn7LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHj3VYs6PiCq MVLHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDLRkBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIGLGR{9HWmGucHjhM3BETlRiYX\0[ZIhQTZiaILzJIJ6KEOnbHzUbZRmei2kbIXlJIF{e2G7LDDJR|UxRTBwNEegcm0> NVLiWYw1OjRzMUG5OFI>
Chinese hamster R2 cells MmK2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLNbYg6PiCq MWXHdo94fGhiaX7obYJqfGmxbjDv[kBEcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeIVzNWKudXWgZZN{[XluIFnDOVA:OC5yNUeg{txO MVSyOFEyOTl2Mh?=

... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 477.47
Formula

C23H23N7O5

CAS No. 146464-95-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02594267 Recruiting Peripheral T-Cell Lymphoma (PTCL) Spectrum Pharmaceuticals, Inc October 2015 Phase 1
NCT02013362 Active, not recruiting Peripheral T-cell Lymphoma Mundipharma K.K. December 2013 Phase 1|Phase 2
NCT01947140 Recruiting Lymphoid Malignancies|Multiple Myeloma|Lymphoma|Hodgkin Lymphoma|Non-hodgkin Lymphoma Jennifer Amengual|Columbia University September 2013 Phase 1|Phase 2
NCT01482962 Active, not recruiting Relapsed Peripheral T-Cell Lymphoma|Refractory Peripheral T-Cell Lymphoma Millennium Pharmaceuticals, Inc.|Takeda June 2012 Phase 3
NCT01626664 Active, not recruiting Adult T-cell Leukemia-Lymphoma Kyowa Hakko Kirin Pharma, Inc.|Kyowa Kirin Pharmaceutical Development, Inc. June 2012 Phase 2
NCT01532011 Completed Advanced Cancers|Solid Tumors M.D. Anderson Cancer Center March 2012 Phase 1

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.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID