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10-Propargyl-10-deazaaminopterin(CAS#146464-95-1)

Chemical Property:

Molecular Formula C23H23N7O5
Molar Mass 477.47
Density 1.471±0.06 g/cm3(Predicted)
Melting Point 215 °C(dec.)
Water Solubility Insoluble in water
Solubility Soluble in DMSO (28 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/
Appearance powder to crystal
Color White to Light yellow
pKa 3.53±0.10(Predicted)
Storage Condition 2-8°C
Refractive Index 1.703
Use An inhibitor of DHFR (dihydrofolate reductase)
In vitro study Pralatrexate and bortezomib showed a wide range of concentration-and time-dependent inhibitory effects on T-type lymphoma cell lines. Pralatrexate and bortezomib in combination induce potent apoptosis and caspase activation. Pralatrexate significantly regulated expression of p27,NOXA,HH3, and RFC-1 by Western blot analysis. Pralatrexate improves cellular delivery via RFC-1 and has greater intracellular drug retention through enhanced polyglutamylated conjugate production. Pralatrexate is thought to exert its pharmacological effects primarily by inhibiting DHFR, with IC 50 in the picomolar range. Pralatrexate has superior intracellular transport through reduced folate carrier and enhanced intracellular accumulation of polyglutamic acid. Pralatrexate exhibits antitumor activity, which is superior to the activity of other antifolates. The enhanced activity of Pralatrexate relative to methotrexate (MTX) is due to its more rapid transport and speed of polyglutamation, the former being less important when the vector is saturated.
In vivo study Pralatrexate treatment resulted in treatment-related toxicities in the MV522 mouse model, such as significant wasting before death in some animals, however, the remaining mice all lost weight by 35 days after dosing.

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10-Propargyl-10-deazaaminopterin(CAS#146464-95-1)

introduce
Pralatrexate is an antifolate agent that is structurally similar to folic acid and acts on some cell lines with IC50s below 300 nM.
Brief introduction
10-Parinpropyl-10-desazaminopterin is an organic compound, often abbreviated as EZA. The following is an introduction to the nature, use, manufacturing method and safety information of EZA:

Quality:
- EZA is a white crystalline solid.
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- EZA has high thermal stability and can be stored and used at high temperatures.

Use:

Method:
- The preparation of EZA is usually carried out by chemical synthesis.
- A common preparation method is to react 2,4,5-triaminopyrimidine with n-butynol to obtain EZA.

Safety Information:
- EZA has some toxicity and should be handled with care.
- Appropriate safety measures such as wearing protective gloves, goggles, and protective clothing are required when using and operating EZA.
- EZA should be kept away from ignition sources and oxidants, and avoid contact with flammable materials. During operation, care should be taken to prevent it from inhaling, touching the skin and eyes to avoid adverse reactions.


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