Talotrexin

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Talotrexin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

113857-87-7

PT523

Talotrexin (PT523) 是一种 Aminopterin (HY-14518) 的类似物，是一种非聚谷氨酸化的经典抗叶酸剂 (antifolate)。 Talotrexin 是一种RFC(还原型叶酸载体)的特异性抑制剂，可选择性地抑制 RFC 转运。Talotrexin 通过靶向DHFR抑制肿瘤生长显示出抗肿瘤活性。

生物活性

Talotrexin (PT523), an analog ofAminopterin(HY-14518), is a nonpolyglutamatable classicantifolate. Talotrexin is aRFC (reduced folate carrier)specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targetingDHFRto inhibit tumor growth^[1]^[2].

体外研究
(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]。

体内研究
(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 withPaclitaxel(HY-B0015, 7.5 mg/kg)
Administration:	IV injection, once weekly for 4 weeks
Result:	Inhibited A549 tumor growth. At Day 30, changes in tumor volumes of the groups treated with talotrexin at 25 and 35 mg/kg were significantly lower than that of the control group.

分子量

573.56

Formula

C₂₇H₂₇N₉O₆

CAS 号

113857-87-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.