Piritrexim

SKU: orb1702937

Description

Piritrexim (BW 301U) is a lipophilic, orally bioavailable inhibitor of dihydrofolate reductase. It has been investigated in preclinical and clinical research for uroepithelial carcinoma and metastatic breast cancer, though its development is noted for associated pulmonary toxicity.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 72732-56-0
• MW: 325.37
• Purity: 99.68% (May vary between batches)
• Formula: C₁₇H₁₉N₅O₂
• SMILES: CC=1C2=C(N=CC1CC3=C(OC)C=CC(OC)=C3)N=C(N)N=C2N
• Target: DHFR

Bioactivity

• Target IC50:
  Walker 256 cells:0.008 uM(ED50)
• In Vivo:
  Piritrexim (25-mg/m2/dose; oral) occurred the myelosuppression and mucositis in 4 of 4 patients but in none of the patients treated at the 15- and 20-mg/m2/dose levels. Piritrexim (20 mg/m2/dose; oral) was rapidly absorbed, with the median time to peak level occurring 1.5 h after an oral dose, and the area under the concentration-time curve (AUC) was linearly related to the dose administered. Trough plasma piritrexim concentration strongly correlated with DLT (P = 0.0016). A trough plasma piritrexim concentration greater than 0.5 microM appeared to be predictive of toxicity. Eleven of 15 patients with trough concentrations exceeding this threshold experienced DLTs.
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• In Vitro:
  Piritrexim (0.1 to 1.0 microM) was able to inhibit the replication of T.gondii in a mouse peritoneal macrophage model. The addition of sulfadiazine, which alone was ineffective, to piritrexim allowed inhibition of T.gondii replication at lower concentrations of piritrexim than when piritrexim was used alone.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DHFR, BW 301U, Piritrexim

Compound Identifiers

PubChem CID

54369