Oxamniquine (CAS 21738-42-1) is a synthetic anthelmintic compound of the tetrahydroquinoline class, widely used in antiparasitic research and drug repurposing programs. Also known as PF-00344645, it serves as a validated reference compound for schistosomiasis studies and broader pharmacological investigations.
Oxamniquine is a semisynthetic small molecule with molecular formula C₁₄H₂₁N₃O₃ and Oxamniquine molecular weight of 279.33 g/mol. The Oxamniquine chemical structure is built around a tetrahydroquinoline scaffold with a nitro group at position 7 and hydroxymethyl and isopropylaminomethyl substituents. Researchers analyze the Oxamniquine structure to better understand its receptor engagement profile and bioactivation pathway. The compound is registered under CAS 21738-42-1 and well-characterized by analytical and crystallographic data.
Application of Oxamniquine
Oxamniquine is primarily used in studies targeting Schistosoma mansoni infection and antiparasitic drug discovery. Beyond parasitology, it is investigated in oncology-related models, particularly in thyroid cancer and retinoblastoma research, supporting its use in drug repurposing workflows. Scientists apply PF-00344645 across early-stage screening and translational research where selective bioactivation mechanisms are under evaluation.
In Vitro
In vitro studies show that Oxamniquine inhibits DNA, RNA, and protein synthesis in susceptible S. mansoni strains. In cancer cell models, the compound suppresses proliferation, reduces ATP production, and disrupts Akt/AMPK/mTOR signaling. It also enhances chemosensitivity in retinoblastoma cells through mitochondria-dependent mechanisms.
In Vivo
In vivo, Oxamniquine demonstrates meaningful activity in murine infection and tumor models. Studies confirm significant reduction in parasite burden, particularly in combination with praziquantel. In oncological models, it suppresses tumor growth and inhibits angiogenesis, with pharmacokinetic data showing rapid oral absorption and high biliary distribution.
Biochemical and Physiological Actions
Oxamniquine is bioactivated by a parasite-specific sulfotransferase into an electrophilic intermediate that alkylates helminth DNA — explaining both its potency and resistance in sulfotransferase-deficient strains. At the physiological level, it induces worm paralysis and displacement to the liver. Additional actions include inhibition of nucleic acid synthesis and mitochondrial complex III activity.
Features and Benefits of Oxamniquine
Oxamniquine (PF-00344645, CAS 21738-42-1) offers a well-documented activity profile suitable for diverse research applications:
- selective bioactivation via parasite-specific sulfotransferase pathway;
- validated activity in antiparasitic and antitumor experimental models;
- well-characterized structure supported by crystallographic data;
- suitable for in vitro screening and in vivo translational studies.
When sourced as EBC-26423, the compound is supported by quality control standards and analytical validation.
