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    Pralatrexate (racemic)
    Pralatrexate (racemic)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0848
    CAS #: 146464-95-1 Purity ≥98%

    Description: Pralatrexate (also known as Folotyn), an antifolate which is structurally a folate analog, is a potent and selective inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

    References: Clin Cancer Res. 2010 Jul 15;16(14):3648-58; Cancer Chemother Pharmacol. 2009 Oct;64(5):993-9. 

    Related CAS: 146464-95-1 (racemic); 1320211-69-5 (S-isomer); 1320211-70-8 (R-isomer)

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    Molecular Weight (MW)477.47
    FormulaC23H23N7O5
    CAS No.146464-95-1(racemic); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 28 mg/mL (58.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info
    Chemical Name: N -(4-{1-[(2,4-diaminopteridin-6-yl)methyl]but-3-yn-1-yl}benzoyl)-L-glutamic acid
    InChi Key: OGSBUKJUDHAQEA-WMCAAGNKSA-N
    InChi Code: InChI=1S/C23H23N7O5/c1-2-3-14(10-15-11-26-20-18(27-15)19(24)29-23(25)30-20)12-4-6-13(7-5-12)21(33)28-16(22(34)35)8-9-17(31)32/h1,4-7,11,14,16H,3,8-10H2,(H,28,33)(H,31,32)(H,34,35)(H4,24,25,26,29,30)/t14?,16-/m0/s1
    SMILES Code: O=C(O)CC[[email protected]@H](C(O)=O)NC(C1=CC=C(C(CC2=NC3=C(N)N=C(N)N=C3N=C2)CC#C)C=C1)=O 
    SynonymsPDX; Pralatrexate; 10-Propargyl-10-deazaaminopterin; trade name: Folotyn. 


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    In Vitro

    In vitro activity: 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


    Cell Assay: Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Based on preclinical studies, researchers believe that Pralatrexate selectively enters cells expressing reduced folate carrier type 1 (RFC-1), a protein that is overexpressed on certain cancer cells compared to normal cells. 

    In VivoPralatrexate 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.
    Animal modelMV522 mice
    Formulation & DosageN/A
    ReferencesClin Cancer Res. 2010 Jul 15;16(14):3648-58; Cancer Chemother Pharmacol. 2009 Oct;64(5):993-9. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Pralatrexate
    A short-term uptake of radiolabeled antifolates in NCI-H460 cells Drugs were dosed for 15 or 60 min. White bars cells incubated with radiolabeled drug only, black bars cells incubated with radiolabeled drug plus excess unlabeled drug. Cancer Chemother Pharmacol.2009 Oct;64(5):993-9.
     
    Pralatrexate
    Differential activity of the antifolates on tumor volume and body weight in NCI-H460 and MV522 human tumor xenografts. Cancer Chemother Pharmacol. 2009 Oct;64(5):993-9.
     
    Pralatrexate
    Inhibition of DHFR activity by pralatrexate in a cell-free system. Cancer Chemother Pharmacol. 2009 Oct;64(5):993-9. 


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