磷酸氟达拉滨 T6501

Product Introduction
Bioactivity


英文名: Fludarabine Phosphate

描述: Fludarabine Phosphate (NSC 312887 Phosphate) 是一种腺苷和脱氧腺苷类似物，与 dATP 竞争，并入到 DNA，可以抑制 DNA 聚合酶 α、核糖核苷酸还原酶和 DNA 引发酶，从而中断 DNA 合成并抑制肿瘤细胞生长。

细胞实验: Cells are incubated with Fludarabine Phosphate for 5 hr and washed twice with drug-free warm medium. 800 cells are mixed with 1.3 mL of 0.25% soft agar in Dulbecco's medium supplemented with 20% fetal bovine serum (pre-warmed to 37 ℃) and incubated in a tissue culture dish for 10 days (humidified 5% CO2 , 37 ℃). At the end of the incubation period, colonies of more than 40 cells are scored under a microscope. The cytotoxic effect of the drugs is expressed as a percentage of survival relative to that of untreated control cells.(Only for Reference)

体外活性: Fludarabine Phosphate的最大耐受剂量为234 mg/kg.Fludarabine对小鼠的LD50为375 mg/kg.Fludarabine Phosphate对于无肿瘤的小鼠有毒性.在携带P388白血病的小鼠中,Fludarabine Phosphate可诱导细胞存活治疗的数量减少,寿命更大比例地增加110％,平均存活时间增加.

体内活性: Fludarabine Phosphate完全抑制DNA聚合酶α/δ（Ki：1.1/1.3 μM）。在体外,DNA聚合酶δ可将Fludarabine Phosphate从结合的DNA上切除。Fludarabine Phosphate与三磷酸脱氧腺苷竞争性地结合到延伸DNA链的A位点,使DNA链延伸的终止人DNA聚合酶α比δ更能将Fludarabine Phosphate结合到DNA中。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 68 mg/mL (186.2 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 2 mg/mL (5.47 mM)


关键字: NSC 118218 | Inhibitor | NSC-312887 Phosphate | Fludarabine Phosphate | NSC312887 Phosphate | Fludarabine | inhibit | NSC118218 | Nucleoside Antimetabolite/Analog | Apoptosis | NSC-118218

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相关库: Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途