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

Modify Date: 2024-04-02 12:19:39

Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]- Structure
Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]- structure
Common Name Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]-
CAS Number 113857-87-7 Molecular Weight 573.56000
Density 1.51g/cm3 Boiling Point N/A
Molecular Formula C27H27N9O6 Melting Point N/A
MSDS N/A Flash Point N/A

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


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].

 Names

Name 2-[[4-carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acid

  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
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