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Purity: ≥98%
Pralatrexate (PDX; trade name 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. Pralatrexate has been approved by FDA to treat a certain type of cancer called peripheral T-Cell lymphoma-PTCL.
| ln Vitro |
When administered to different T lymphoma cell lines, pralatrexate (100 pM-200 μM; 48-72 h) demonstrates cytotoxicity that is dependent on both concentration and time. The following are the IC50 values at 48 and 72 hours: 1.1 and 2.5 nM for H9 cells; 1.7 and 2.4 nM for P12 cells; 3.2 and 4.2 nM for CEM cells; 5.5 and 2.7 nM for PF-382 cells; 1 and 1.7 nM for KOPT-K1 cells; 97.4 and 1.2 nM for DND-41 cells; and 247.8 nM and 0.77 nM for HPB-ALL cells. After 48 hours of treatment, HH cells showed some resistance, with an IC50 of 2.8 nM at 72 hours [1]. Treatment with pralidoxate (2-5.5 nM; 48-72 h; H9, HH, P12, and PF382 cells) results in strong apoptosis and caspase-8 and caspase-9 activation [1]. Treatment of H9 and P12 cells with pralitrexate (3 nM; 16–48 hours) dramatically raises p27 levels and promotes the accumulation of inducible folate carrier type 1 (RFC-1) in the cells [1].
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| ln Vivo |
In comparison to either drug alone, the combination of Bortezomib (0.5 mg/kg) and Pralatrexate (15 mg/kg; intraperitoneal injection; on days 1, 4, 8, and 11; SCID-beige mice) increased effectiveness [1].
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: T-lymphoma cell lines Tested Concentrations: 100 pM-200 µM Incubation Duration: 48 hrs (hours), 72 hrs (hours) Experimental Results: demonstrated concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. Apoptosis Analysis[1] Cell Types: H9, HH, P12 and PF382 cells Tested Concentrations: 2 nM, 3 nM, 4 nM, 5.5 nM Incubation Duration: 48 hrs (hours), 72 hrs (hours) Experimental Results: Induced potent apoptosis and caspase activation. Western Blot Analysis[1] Cell Types: H9 and P12 cells Tested Concentrations: 3 nM Incubation Duration: 16 hrs (hours), 24 hrs (hours), 48 hrs (hours) Experimental Results: Clearly increased p27 levels and increased the accumulation of RFC-1 in cells. |
| Animal Protocol |
Animal/Disease Models: SCID-beige mice (5-7weeks old) injected with HH cells[1]
Doses: 15 mg/kg Route of Administration: intraperitoneal (ip)injection; on days 1, 4, 8, and 11 Experimental Results: demonstrated superior efficacy in T-cell malignancies. |
| References |
[1]. Enrica Marchi, et al. Pralatrexate Is Synergistic With the Proteasome Inhibitor Bortezomib in in Vitro and in Vivo Models of T-cell Lymphoid Malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58.
[2]. Francine Foss, et al. Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study. Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. [3]. Karen Kelly, et al. Randomized Phase 2b Study of Pralatrexate Versus Erlotinib in Patients With Stage IIIB/IV Non-Small-Cell Lung Cancer (NSCLC) After Failure of Prior Platinum-Based Therapy. J Thorac Oncol. 2012 Jun;7(6):1041-8. [4]. F M Sirotnak, et al. A New Analogue of 10-deazaaminopterin With Markedly Enhanced Curative Effects Against Human Tumor Xenografts in Mice. Cancer Chemother Pharmacol. 1998;42(4):313-8. |
| Molecular Formula |
C23H23N7O5
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| Molecular Weight |
477.47
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| CAS # |
146464-95-1
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| Related CAS # |
(R)-Pralatrexate;1320211-70-8
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| SMILES |
O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(C(CC2=NC3=C(N)N=C(N)N=C3N=C2)CC#C)C=C1)=O
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| InChi Key |
OGSBUKJUDHAQEA-WMCAAGNKSA-N
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| 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
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| Chemical Name |
N -(4-{1-[(2,4-diaminopteridin-6-yl)methyl]but-3-yn-1-yl}benzoyl)-L-glutamic acid
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| Synonyms |
PDX; Pralatrexate; 10-Propargyl-10-deazaaminopterin; trade name: Folotyn.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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