Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
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 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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 )
You can also refer to dose conversion for different animals. More
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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