Fludarabine phosphate (Synonyms: 磷酸氟达拉滨; NSC 118218 phosphate)

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Data Sheet SDS COA 产品使用指南

摩尔计算器

Fludarabine phosphate (NSC 118218 phosphate) 是一种腺苷和脱氧腺苷类似物，与 dATP 竞争，并入到 DNA，导致 DNA 合成受阻。

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Fludarabine phosphate Chemical Structure

CAS No. : 75607-67-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥798	In-stock
1 mg	￥226	In-stock
5 mg	￥400	In-stock
10 mg	￥600	In-stock
50 mg	￥1800	In-stock
100 mg	￥2697	In-stock
200 mg		询价
500 mg		询价

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	2 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human M-HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human M-HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
HL-60	IC₅₀	0.09 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
K562	IC₅₀	0.4 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
KG-1	IC₅₀	0.15 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
MCF7	IC₅₀	0.13 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
MOLT-3	IC₅₀	0.95 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
Raji	IC₅₀	0.4 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human Raji cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
Skut1B	IC₅₀	6 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
ZR-75-1	IC₅₀	0.6 μM Compound: fludarabine phosphate, F-ara-AMP	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]

体外研究
(In Vitro)

Fludarabine phosphate significantly reduces the cell viability in a dose-dependent manner. Fludarabine phosphate exhibits no effect in all tested concentrations when combined with either PBS or control vector, ACE-GFP. Fludarabine phosphate causes a significant decrease in cell viability for 24 h after exposure to ACE-PNP when compared to PBS and ACE-GFP at concentrations of 2.5, 5 and 10 μg/mL^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

F-araAMP (100 mg/kg given 15 times, 167 mg/kg given 9 times, or 250 mg/kg given 3 times, i.p.) leads to complete regressions of all tumors and cures of all mice. Parental D54 tumors (i.e. without E. coli PNP) are not sensitive to treatment with F-araAMP. Intratumoral injection of Ad/PNP followed by IT F-araAMP can elicit a substantial regressive effect on otherwise refractory solid tumors in a fashion substantially superior to viral PNP transduction followed by systemic prodrug administration^[1]. The comparison of ACE-GFP/fludarabine phosphate with ACE-GFP/PBS demonstrats that fludarabine phosphate alone has no growth inhibitory activity on KU-19-19 tumors^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

365.21

Formula

C₁₀H₁₃FN₅O₇P

CAS 号

75607-67-9

性状

固体

颜色

White to off-white

中文名称

磷酸氟达拉滨；2-氟阿糖腺苷酸；氟达拉宾碱；氟达那苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (273.82 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 5 mg/mL (13.69 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7382 mL	13.6908 mL	27.3815 mL
5 mM	0.5476 mL	2.7382 mL	5.4763 mL
10 mM	0.2738 mL	1.3691 mL	2.7382 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： phosphate buffer Saline
Solubility: 20 mg/mL (54.76 mM); 澄清溶液; 超声助溶
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.85 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.85 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.85 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 18.33 mg/mL (50.19 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.77%

选择批次：

Data Sheet (629 KB) SDS (418 KB)

COA (290 KB) RP-HPLC (116 KB) MS (133 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Sorscher EJ, et al. In vivo antitumor activity of intratumoral fludarabine phosphate in refractory tumors expressing E. coli purine nucleoside phosphorylase. Cancer Chemother Pharmacol. 2012 Aug;70(2):321-9. [Content Brief]

[2]. Kikuchi E, et al. Delivery of replication-competent retrovirus expressing Escherichia coli purine nucleoside phosphorylase increases the metabolism of the prodrug, fludarabine phosphate and suppresses the growth of bladder tumor xenografts. Cancer Gene Th [Content Brief]

Cell Assay ^[2]	Briefly, 2×10³ KU-19-19 cells are seeded in each well of 96-well plates and allowed to grow overnight. Cells are then exposed to PBS, ACE-GFP or ACE-PNP for 3 h. Twenty-four hours post-infection, the cells are treated with various concentrations of fludarabine phosphate. After the 24-h incubation, cytotoxicity is determined by using WST-1; 4-[3-(4-iodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]-1,3-benzene disulfonate. The absorbance value is determined at 450 nm by a microplate reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Parental and E. coli PNP expressing D54MG (human glioma) tumor cells (2×10⁷ cells) are injected subcutaneously into the flanks of nude mice (nu/nu). D54 tumor cells stably transduced with E. coli PNP are prepared as described previously. Tumors are measured with calipers and an estimate of the weight calculated using the equation, (length × width²)/2=mm³, and converted to mg assuming unit density. Unless stated otherwise, therapeutic drugs and the adenoviral vector expressing E. coli PNP (Ad/PNP), or vehicle controls are injected into D54 tumors in 150 μL volumes by 8 separate injections of approximately 20 μL each in an effort to evenly distribute the administered agent. At least 6 mice are studied in each treatment group. Mice are monitored daily and body weights and tumor dimensions collected twice weekly. T-C (tumor growth delay) is determined as the difference in median days to 2 doublings (median days to 600 mg for the D54 and DU145 (human prostate cancer) analysis) between drug-treated and vehicle-treated groups. For the NIH-H322M (human non-small cell lung cancer) study, because of tumor proliferation characteristics, total growth inhibition (TGI) is used as the evaluation point. TGI is equal to the control group mean delta minus the treated group mean delta divided by the control group mean delta, where delta is the change in tumor weight for each animal between day 36 and day 59. The time to the evaluation point for each animal is used as the end point for the student's t-test, Mann-Whitney rank sum test, or a life table analysis in order to statistically compare growth data between treatment groups. All key results are repeated under similar conditions and findings confirmed. Treatments are initiated when tumors are 250 to 300 mg (appr 1-1.5% of total animal weight). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Sorscher EJ, et al. In vivo antitumor activity of intratumoral fludarabine phosphate in refractory tumors expressing E. coli purine nucleoside phosphorylase. Cancer Chemother Pharmacol. 2012 Aug;70(2):321-9. [Content Brief] [2]. Kikuchi E, et al. Delivery of replication-competent retrovirus expressing Escherichia coli purine nucleoside phosphorylase increases the metabolism of the prodrug, fludarabine phosphate and suppresses the growth of bladder tumor xenografts. Cancer Gene Th [Content Brief]

Fludarabine phosphate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.7382 mL	13.6908 mL	27.3815 mL	68.4538 mL
	5 mM	0.5476 mL	2.7382 mL	5.4763 mL	13.6908 mL
	10 mM	0.2738 mL	1.3691 mL	2.7382 mL	6.8454 mL
DMSO	15 mM	0.1825 mL	0.9127 mL	1.8254 mL	4.5636 mL
	20 mM	0.1369 mL	0.6845 mL	1.3691 mL	3.4227 mL
	25 mM	0.1095 mL	0.5476 mL	1.0953 mL	2.7382 mL
	30 mM	0.0913 mL	0.4564 mL	0.9127 mL	2.2818 mL
	40 mM	0.0685 mL	0.3423 mL	0.6845 mL	1.7113 mL
	50 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3691 mL
	60 mM	0.0456 mL	0.2282 mL	0.4564 mL	1.1409 mL
	80 mM	0.0342 mL	0.1711 mL	0.3423 mL	0.8557 mL
	100 mM	0.0274 mL	0.1369 mL	0.2738 mL	0.6845 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fludarabine75607-67-9NSC 118218磷酸氟达拉滨2-氟阿糖腺苷酸氟达拉宾碱氟达那苷NSC118218NSC-118218Nucleoside Antimetabolite/AnalogApoptosisInhibitorinhibitorinhibit

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Fludarabine phosphate (Synonyms: 磷酸氟达拉滨; NSC 118218 phosphate)

Customer Review

Other Forms of Fludarabine phosphate:

MCE 顾客使用本产品发表的 4 篇科研文献

Fludarabine phosphate 相关产品

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•同靶点产品:

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参考文献

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Fludarabine phosphate 相关分类

完整储备液配制表

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Fludarabine phosphate (Synonyms: 磷酸氟达拉滨; NSC 118218 phosphate)

Customer Review

Other Forms of Fludarabine phosphate:

Fludarabine phosphate 相关抗体

MCE 顾客使用本产品发表的 4 篇科研文献

Fludarabine phosphate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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实验参考方法

纯度 & 产品资料

参考文献

Fludarabine phosphate 相关抗体:

摩尔计算器

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Fludarabine phosphate 相关分类

完整储备液配制表

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