| Identification | Back Directory | [Name]
2-[[(4S)-4-carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoy l]amino]butyl]carbamoyl]benzoic acid | [CAS]
113857-87-7 | [Synonyms]
PT-523
talotrexin
NYQPLPNEESYGNO-IBGZPJMESA-N
N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine
(S)-2-[4-[(2,4-Diaminopteridin-6-yl)methylamino]benzoylamino]-5-(2-carboxybenzoylamino)valeric acid
2-[[(4S)-4-carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoy l]amino]butyl]carbamoyl]benzoic acid
Benzoic acid, 2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]- | [Molecular Formula]
C27H27N9O6 | [MOL File]
113857-87-7.mol | [Molecular Weight]
573.56 |
| Chemical Properties | Back Directory | [Melting point ]
208 °C (decomp) | [density ]
1.510±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
3.503±0.36(predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | 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. DOI:10.1038/s41598-021-85818-x
[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). |
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