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Pralatrexate

Catalog No. T6120 CAS 146464-95-1

Synonyms: 10-炔丙基-10-去氮杂氨基蝶呤, 10-Propargyl-10-deazaaminopterin, 普拉曲沙, Folotyn

Pralatrexate 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

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pralatrexate 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	10-炔丙基-10-去氮杂氨基蝶呤, 10-Propargyl-10-deazaaminopterin, 普拉曲沙, Folotyn
Molecular Weight	477.481
Formula	C23H23N7O5
CAS No.	146464-95-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 27 mg/mL (56.5 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

Anti-Cancer Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library DNA Damage & Repair Compound Library Anti-Metabolism Disease Compound Library Cell Cycle Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library

Related Products

Related compounds with same targets

Metoprine Aminopterin Calcium N5-methyltetrahydrofolate Levomefolate calcium Pemetrexed disodium hemipenta hydrate Pralatrexate Proguanil hydrochloride Diaveridine

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Keywords

Pralatrexate 146464-95-1 DNA损伤和修复代谢蛋白酪氨酸激酶凋亡细胞周期 Antifolate Apoptosis DHFR TAM Receptor 10-Propargyl-10-deazaaminopterin antitumor folylpolyglutamate cytotoxicity inhibit Inhibitor RFC-1 dihydrofolate p27 reductase synthetase Folotyn inhibitor

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