Talotrexin  (Synonyms: PT523)

Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth^[1][2].

Talotrexin shows no significant PCFT or FRα inhibitory activity^[1].
Talotrexin (1-1000 nM) inhibits proliferation of R1-11/Tet-on-RFC HeLa cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Talotrexin (0-35 mg/kg, IV injection, once weekly for 4 weeks) alone or combined with Paclitaxel (HY-B0015, 7.5 mg/kg) inhibits A549 tumor growth in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

573.56

C₂₇H₂₇N₉O₆

113857-87-7

NC1=NC(N)=NC2=C1N=C(CNC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCCNC(C4=C(C=CC=C4)C(O)=O)=O)=O)C=N2

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• [1]. O'Connor C, et al. Folate transporter dynamics and therapy with classic and tumor-targeted antifolates. Sci Rep. 2021 Mar 18;11(1):6389.  [Content Brief]

  [2]. Choy G S, et al. Combination talotrexin (PT-523) with paclitaxel in A549 non-small cell lung cancer (NSCLC) athymic nude mice xenografts[J]. Cancer Research, 2007, 67(1_Annual_Meeting).