1. Cell Cycle/DNA Damage Autophagy Apoptosis
  2. Nucleoside Antimetabolite/Analog Autophagy Apoptosis
  3. Clofarabine

Clofarabine  (Synonyms: 氯法拉滨)

目录号: HY-A0005 纯度: 99.88%
COA 产品使用指南

Clofarabine是一种用于癌症研究的核苷类似物,是一种有效的核糖核苷酸还原酶 (ribonucleotide reductase) 抑制剂 (IC50=65 nM)。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Clofarabine Chemical Structure

Clofarabine Chemical Structure

CAS No. : 123318-82-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥567
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5 mg ¥321
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10 mg ¥515
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25 mg ¥992
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50 mg ¥1588
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100 mg ¥2223
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Other Forms of Clofarabine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
0.086 μM
Compound: Clofarabine
Cytostatic activity against human A549 cells after 5 days by SRB assay
Cytostatic activity against human A549 cells after 5 days by SRB assay
[PMID: 21711054]
A549 IC50
8 μM
Compound: 1, clofarabine
Cytostatic activity against human A549 cells after 48 hrs by MTT assay
Cytostatic activity against human A549 cells after 48 hrs by MTT assay
[PMID: 23820572]
BT-549 GI50
0.065 μM
Compound: Clofarabine
Cytostatic activity against human BT549 cells after 5 days by SRB assay
Cytostatic activity against human BT549 cells after 5 days by SRB assay
[PMID: 21711054]
BT-549 GI50
0.065 μM
Compound: clofarabine
Cytotoxicity against human BT549 cells after 5 days by SRB assay
Cytotoxicity against human BT549 cells after 5 days by SRB assay
[PMID: 19929004]
CCRF-CEM IC50
0.044 μM
Compound: Clofarabine
Cytotoxicity against human CCRF-CEM cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human CCRF-CEM cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 30176535]
DU-145 GI50
0.125 μM
Compound: Clofarabine
Cytostatic activity against human DU145 cells after 5 days by SRB assay
Cytostatic activity against human DU145 cells after 5 days by SRB assay
[PMID: 21711054]
Granta IC50
0.017 μM
Compound: Clofarabine
Cytotoxicity against human Granta cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human Granta cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 30176535]
HCT-116 GI50
0.106 μM
Compound: Clofarabine
Cytostatic activity against human HCT116 cells after 5 days by SRB assay
Cytostatic activity against human HCT116 cells after 5 days by SRB assay
[PMID: 21711054]
HCT-15 GI50
0.18 μM
Compound: Clofarabine
Cytostatic activity against human HCT15 cells after 5 days by SRB assay
Cytostatic activity against human HCT15 cells after 5 days by SRB assay
[PMID: 21711054]
HCT-15 GI50
0.18 μM
Compound: clofarabine
Cytotoxicity against human HCT15 cells after 5 days by SRB assay
Cytotoxicity against human HCT15 cells after 5 days by SRB assay
[PMID: 19929004]
HeLa IC50
50 μM
Compound: 1, clofarabine
Cytostatic activity against human HeLa cells after 48 hrs by MTT assay
Cytostatic activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 23820572]
HL-60 IC50
0.04 μM
Compound: Clofarabine
Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 30176535]
HL-60 IC50
0.1 μM
Compound: 1, clofarabine
Cytostatic activity against human HL60 cells after 48 hrs by MTT assay
Cytostatic activity against human HL60 cells after 48 hrs by MTT assay
[PMID: 23820572]
MCF7 IC50
50 μM
Compound: 1, clofarabine
Cytostatic activity against human MCF7 cells after 48 hrs by MTT assay
Cytostatic activity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 23820572]
MT4 GI50
0.051 μM
Compound: Clofarabine
Cytostatic activity against human MT4 cells after 5 days by SRB assay
Cytostatic activity against human MT4 cells after 5 days by SRB assay
[PMID: 21711054]
NCI-H23 GI50
0.04 μM
Compound: Clofarabine
Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay
Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay
[PMID: 21711054]
NCI-H23 GI50
0.04 μM
Compound: clofarabine
Cytotoxicity against human NCI-H23 cells after 5 days by SRB assay
Cytotoxicity against human NCI-H23 cells after 5 days by SRB assay
[PMID: 19929004]
PC-3 GI50
0.063 μM
Compound: Clofarabine
Cytostatic activity against human PC3 cells after 5 days by SRB assay
Cytostatic activity against human PC3 cells after 5 days by SRB assay
[PMID: 21711054]
PC-3 GI50
0.063 μM
Compound: clofarabine
Cytotoxicity against human PC3 cells after 5 days by SRB assay
Cytotoxicity against human PC3 cells after 5 days by SRB assay
[PMID: 19929004]
RL IC50
0.38 μM
Compound: Clofarabine
Cytotoxicity against human RL cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human RL cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 30176535]
U373-MAGI CC50
243 μM
Compound: Clofarabine
Increase of 5-Aza-C-mediated cytotoxicity against human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs measured after 72 hrs by Celltiter-Glo luminescent cell viability assay (Rvb = 387 uM)
Increase of 5-Aza-C-mediated cytotoxicity against human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs measured after 72 hrs by Celltiter-Glo luminescent cell viability assay (Rvb = 387 uM)
[PMID: 27117260]
U373-MAGI EC50
30.4 μM
Compound: Clofarabine
Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection measu
Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection measu
[PMID: 27117260]
体外研究
(In Vitro)

Clofarabine potently inhibits DNA synthesis. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50 values=0.028-0.29 μM) in a wide variety of leukaemia and solid tumour cell lines[1].
? Clofarabine (0.01-0.1 μM) inhibits proliferation of NB4 cells, which may be related with the down-regulation of Bcl-2 and induction of apoptosis[2].

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

Cell Viability Assay[2]

Cell Line: NB4 cells
Concentration: 0.01-0.1 µM
Incubation Time: 48 hours
Result: Inhibited proliferation of NB4 cells in a concentration-depended manner.

Apoptosis Analysis[2]

Cell Line: NB4 cells
Concentration: 0.01-0.1 µM
Incubation Time: 24 hours
Result: Apoptosis rate increased obviously.

Western Blot Analysis[2]

Cell Line: NB4 cells
Concentration: 0.01-0.1 µM
Incubation Time: 24 hours
Result: Bcl-2 expression decreased obviously.
体内研究
(In Vivo)

Clofarabine (330 mg/kg, after a 7-day treatment) causes the death of mice. Higher mortality rates were observed in daytime treatment groups, while more animals survived in night treatment groups. Significant differences of LD50 are found at various time points especially at 12:00 noon and 12:00 midnight[3].

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

Animal Model: Kunming mice (18-22 g, with equal numbers of male and female mice)[3]
Dosage: 600, 480, 384, 307, 246 mg/kg
Administration: Injected intraperitoneally at 8:00 am, 12:00 noon, 8:00 pm and 12:00 midnight; 7 days continuous administration
Result: LD50s of 8:00 am, 12:00 noon, 8:00 pm, 12:00 midnight were 333.59, 319.73, 362.58 and 366.92 mg/kg, respectively.
Clinical Trial
分子量

303.68

Formula

C10H11ClFN5O3

CAS 号
性状

固体

颜色

White to off-white

中文名称

克罗拉滨;氯法拉滨;克罗他滨;氯伐他滨;氯法拉宾;氯伐拉滨

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 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 50 mg/mL (164.65 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)

* "≥" 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 3.2929 mL 16.4647 mL 32.9294 mL
5 mM 0.6586 mL 3.2929 mL 6.5859 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.85 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.85 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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。
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

g

每只动物的给药体积

μL

动物数量

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: 99.88%

参考文献

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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2929 mL 16.4647 mL 32.9294 mL 82.3235 mL
5 mM 0.6586 mL 3.2929 mL 6.5859 mL 16.4647 mL
10 mM 0.3293 mL 1.6465 mL 3.2929 mL 8.2324 mL
15 mM 0.2195 mL 1.0976 mL 2.1953 mL 5.4882 mL
20 mM 0.1646 mL 0.8232 mL 1.6465 mL 4.1162 mL
25 mM 0.1317 mL 0.6586 mL 1.3172 mL 3.2929 mL
30 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7441 mL
40 mM 0.0823 mL 0.4116 mL 0.8232 mL 2.0581 mL
50 mM 0.0659 mL 0.3293 mL 0.6586 mL 1.6465 mL
60 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
80 mM 0.0412 mL 0.2058 mL 0.4116 mL 1.0290 mL
100 mM 0.0329 mL 0.1646 mL 0.3293 mL 0.8232 mL
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  • 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.

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产品名称:
Clofarabine
目录号:
HY-A0005
需求量: