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Pralatrexate
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。
Pralatrexate图片
CAS NO:146464-95-1
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议

产品名称
10-Propargyl-10-deazaaminopterin
10-炔丙基-10-去氮杂氨基蝶呤
普拉曲沙
Folotyn
产品介绍
Pralatrexate 是一种抗叶酸剂,也是二氢叶酸还原酶抑制剂,Ki值为 13.4 pM。它具有抗肿瘤活性,可研究复发/难治性 T 细胞淋巴瘤。它是叶酰聚谷氨酸合成酶的底物,具有改善的细胞摄取和保留能力。

产品描述

Pralatrexate is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

体外活性

Pralatrexate and bortezomib exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. Pralatrexate shows synergism when combined with bortezomib in all cell lines studied. Pralatrexate also induces potent apoptosis and caspase activation when combined with bortezomib across the panel. Pralatrexate significantly modulates the expression of p27, NOXA, HH3, and RFC-1 as assessed by Western blot assays. [1] Pralatrexate is rationally designed for improved cellular transport via RFC-1, and to have greater intracellular drug retention through the enhanced formation of polyglutamylated conjugates. Pralatrexate is thought to exert its pharmacological effect primarily through inhibition of DHFR, having an IC50 in the picomolar range. [2] Pralatrexate demonstrates superior intracellular transport via the reduced folate carrier, and increased accumulation within cells by enhanced polyglutamylation. Pralatrexate exhibits antitumor activity that is superior to the activity of other antifolates. [3] Pralatrexate's enhanced activity relative to methotrexate (MTX) is due to its much more rapid rate of transport and polyglutamation, the former less important when the carrier is saturated. [4]

体内活性

Pralatrexate treatment results in treatment-related toxicity in MV522 mice models, as determined by significant weight loss in some animals prior to death; however, remaining mice regains all lost weight by Day 35. [2]

Cas No.

146464-95-1

分子式

C23H23N7O5

分子量

477.481

别名

10-Propargyl-10-deazaaminopterin;10-炔丙基-10-去氮杂氨基蝶呤;普拉曲沙;Folotyn

储存和溶解度

Ethanol:<1 mgml
DMSO:27 mg/mL (56.5 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years