Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]-

Names

[ Name ]:
Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]-

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate

[In Vitro]

Talotrexin 未显示出显著的 PCFT 或 FRα 抑制活性[1]。 Talotrexin (1-1000 nM) 可抑制 R1-11/Tet-on-RFC HeLa 细胞的增殖[2]。

[In Vivo]

Talotrexin (0-35 mg/kg，静脉注射，每周一次，持续 4 周) 单独或与Paclitaxel (HY-B0015, 7.5 mg/kg) 联合使用可抑制小鼠 A549 肿瘤的生长[2]。 Animal Model: NSCLC xenografts in athymic female nude mice (6-8 weeks)[2] Dosage: 15, 25, and 35 mg/kg, combined with Paclitaxel (HY-B0015, 7.5 mg/kg) Administration: IV injection, once weekly for 4 weeks Result: Inhibited A549 tumor growth.

[References]

[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.

[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).

Chemical & Physical Properties

[ Density]:
1.51g/cm3

[ Molecular Formula ]:
C₂₇H₂₇N₉O₆

[ Molecular Weight ]:
573.56000

[ Exact Mass ]:
573.20800

[ PSA ]:
248.43000

[ LogP ]:
3.30490

[ Index of Refraction ]:
1.737

Related Compounds

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