store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pralatrexate (10-Propargyl-10-deazaaminopterin) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 448 | 现货 | ||
2 mg | ¥ 636 | 现货 | ||
5 mg | ¥ 996 | 现货 | ||
10 mg | ¥ 1,660 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,190 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 现货 |
产品描述 | Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. |
靶点活性 | Axl (SUM149 cells):0.43 μM, Axl (KPL-4 cells):0.16 μM |
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] |
别名 | Folotyn, 10-炔丙基-10-去氮杂氨基蝶呤, 10-Propargyl-10-deazaaminopterin, 普拉曲沙 |
分子量 | 477.47 |
分子式 | C23H23N7O5 |
CAS No. | 146464-95-1 |
store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27 mg/mL (56.5 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0944 mL | 10.4719 mL | 20.9437 mL | 52.3593 mL |
5 mM | 0.4189 mL | 2.0944 mL | 4.1887 mL | 10.4719 mL | |
10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.2359 mL | |
20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.618 mL | |
50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pralatrexate 146464-95-1 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Tyrosine Kinase/Adaptors DHFR Antifolate TAM Receptor antitumor folylpolyglutamate Folotyn cytotoxicity inhibit Inhibitor 10-炔丙基-10-去氮杂氨基蝶呤 RFC-1 dihydrofolate p27 reductase synthetase 10-Propargyl-10-deazaaminopterin 普拉曲沙 inhibitor