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Pralatrexate

Catalog No. T6120 CAS 146464-95-1

Synonyms: Folotyn, 10-Propargyl-10-deazaaminopterin

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

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Pralatrexate, CAS 146464-95-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 172.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 98.56%

Purity: 98.12%

Purity: 94.32%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.
Targets&IC50	Axl (SUM149 cells):0.43 μM, Axl (KPL-4 cells):0.16 μM
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]
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]

Synonyms	Folotyn, 10-Propargyl-10-deazaaminopterin
Molecular Weight	477.47
Formula	C23H23N7O5
CAS No.	146464-95-1

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27 mg/mL (56.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Marchi E, et al. Clin Cancer Res, 2010, 16(14), 3648-3658. 2. Izbicka E, et al. Cancer Chemother Pharmacol, 2009, 64(5), 993-999. 3. Molina JR, et al. IDrugs, 2008, 11(7), 508-521. 4. Visentin M, et al. Cancer Chemother Pharmacol, 2013, 72(3), 597-606.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Drug Library Pediatric Drug Library Bioactive Compounds Library Max

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Keywords

Pralatrexate 146464-95-1 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Tyrosine Kinase/Adaptors DHFR Antifolate TAM Receptor antitumor folylpolyglutamate Folotyn cytotoxicity inhibit Inhibitor RFC-1 dihydrofolate p27 reductase synthetase 10-Propargyl-10-deazaaminopterin inhibitor

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