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Piritrexim

Catalog No. T24644 CAS 72732-56-0

Synonyms: BW 301U

Piritrexim (BW 301U) is an orally available fat-soluble dihydrofolate reductase inhibitor with pulmonary toxicity used in the study of uroepithelial carcinoma and metastatic breast cancer.

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Piritrexim, CAS 72732-56-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 350.00
5 mg	In stock	$ 970.00
25 mg	In stock	$ 1,590.00
50 mg	In stock	$ 1,980.00

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Purity: 99.68%

Purity: 99.13%

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Description	Piritrexim (BW 301U) is an orally available fat-soluble dihydrofolate reductase inhibitor with pulmonary toxicity used in the study of uroepithelial carcinoma and metastatic breast cancer.
Targets&IC50	Walker 256 cells:0.008 uM(ED50)
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.[5]
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.[6] 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.[6]

Synonyms	BW 301U
Molecular Weight	325.37
Formula	C17H19N5O2
CAS No.	72732-56-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Sigel CW, et al. Preclinical biochemical pharmacology and toxicology of piritrexim, a lipophilic inhibitor of dihydrofolate reductase. NCI Monogr. 1987;(5):111-120. 2. Rosowsky A, et al. 2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity. J Med Chem. 1994;37(26):4522-4528. 3. de Vries EG, et al. A phase II and pharmacokinetic study with oral piritrexim for metastatic breast cancer. Br J Cancer. 1993;68(3):641-644. 4. Lassiter LK, et al. Phase II open-label study of oral piritrexim in patients with advanced carcinoma of the urothelium who have experienced failure with standard chemotherapy. Clin Genitourin Cancer. 2008;6(1):31-35. 5. Kovacs JA, et al. Potent antipneumocystis and antitoxoplasma activities of piritrexim, a lipid-soluble antifolate. Antimicrob Agents Chemother. 1988;32(4):430-433. 6. Adamson PC, et al. Pediatric phase I trial, pharmacokinetic study, and limited sampling strategy for piritrexim administered on a low-dose, intermittent schedule. Cancer Res. 1992;52(3):521-524. 7. Grivsky EM, et al. Synthesis and antitumor activity of 2,4-diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidine. J Med Chem. 1980;23(3):327-329.

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Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Piritrexim 72732-56-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR BW 301U inhibitor inhibit

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