Pralatrexate

SKU: orb1301055

Description

Pralatrexate

Research Area

Cell Biology, Metabolism Research, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 146464-95-1
• MW: 477.47
• Purity: 98.56%
• Formula: C₂₃H₂₃N₇O₅
• SMILES: Nc1nc(N)c2nc(CC(CC#C)c3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)cnc2n1
• Target: Antifolate,DHFR,TAM Receptor,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.19 mM);DMSO:250 mg/mL (523.59 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Axl (KPL-4 cells):0.16 μM|Axl (SUM149 cells):0.43 μM
• 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.
• 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 acros the panel. Pralatrexate significantly modulate 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 throug 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 vi 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 whe the carrier is saturated.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

folylpolyglutamate, Folotyn, Inhibitor, inhibit, p27, cytotoxicity, dihydrofolate, DHFR, Antifolate, antitumor, Apoptosis, AXL, 10-Propargyl-10-deazaaminopterin, synthetase, TAM Receptor, TAMReceptor, RFC-1, reductase, Pralatrexate

Compound Identifiers

PubChem CID

148121