Molecular Weight(MW): 477.47
Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.
Purity & Quality Control
Choose Selective DHFR Inhibitors
|Description||Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.|
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.  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.  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.  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. 
|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. |
|In vitro||DMSO||28 mg/mL (58.64 mM)|
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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|
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
We are just wondering if S1497 a racemic mixture or a monomer? Will you please let us know?
S1497 Pralatrexate is S enantiomer.