| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408785-1ml |
1ml |
现货  |
|
| 别名 | 普拉曲沙 (NSC 754230) |
|---|---|
| 英文别名 | N-[4-[1-[(2,4-diamino-6-pteridinyl)methyl]-3-butyn-1-yl]benzoyl]-L-glutamic acid |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Pralatrexate (NSC 754230) |
| 生化机理 | Pralatrexate （NSC 754230）是一种抗叶酸药，结构上属于叶酸类似物。在某些细胞系中，其 IC50 小于 300 nM。Pralatrexate 可诱导肿瘤细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 二氢叶酸还原酶抑制剂 |
| 产品介绍 |
An inhibitor of DHFR (dihydrofolate reductase) Information Pralatrexate (NSC 754230) Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis . 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. 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. 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. 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. In vivo 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. cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | NC1=NC(=C2N=C(CC(CC#C)C3=CC=C(C=C3)C(=O)NC(CCC(O)=O)C(O)=O)C=NC2=N1)N |
| 分子量 | 477.47 |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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