Clofarabine (Synonyms: 氯法拉濱)

目錄號(hào): HY-A0005 純度: 99.88%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Clofarabine是一種用于癌癥研究的核苷類(lèi)似物，是一種有效的核糖核苷酸還原酶 (ribonucleotide reductase) 抑制劑 (IC₅₀=65 nM)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Clofarabine Chemical Structure

CAS No. : 123318-82-1

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥567	In-stock
5 mg	￥321	In-stock
10 mg	￥515	In-stock
25 mg	￥992	In-stock
50 mg	￥1588	In-stock
100 mg	￥2223	In-stock
200 mg		詢(xún)價(jià)
500 mg		詢(xún)價(jià)

or 大包裝詢(xún)價(jià)

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Customer Review

Other Forms of Clofarabine:

Clofarabine (Standard) 詢(xún)價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
•Pharmaceuticals (Basel). 2024 Sep 28;17(10):1295. [Abstract]
•Front Oncol. 2024 Jul 19:14:1440650. [Abstract]
•J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
•Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]

Clofarabine 相關(guān)產(chǎn)品

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生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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].

細(xì)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]

體外研究
(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.

體內(nèi)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 號(hào)

123318-82-1

性狀

固體

顏色

White to off-white

中文名稱(chēng)

克羅拉濱；氯法拉濱；克羅他濱；氯伐他濱；氯法拉賓；氯伐拉濱

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 50 mg/mL (164.65 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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
10 mM	0.3293 mL	1.6465 mL	3.2929 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.85 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.85 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.85 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.88%

選擇批次：

Data Sheet (629 KB) SDS (420 KB)

COA (195 KB) HNMR (240 KB) RP-HPLC (205 KB) LCMS (93 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Peter L Bonate, et al. Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat Rev Drug Discov. 2006 Oct;5(10):855-63. [Content Brief]

[2]. Hai-Bo Liu, et al. [Effect of clofarabine on proliferation and Bcl-2 expression of NB4 cells]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):571-3. [Content Brief]

[3]. Jia-Jie Luan, et al. Dosing-time contributes to chronotoxicity of clofarabine in mice via means other than pharmacokinetics. Kaohsiung J Med Sci. 2016 May;32(5):227-34. [Content Brief]

Clofarabine 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

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:

Clofarabine123318-82-1克羅拉濱氯法拉濱克羅他濱氯伐他濱氯法拉賓氯伐拉濱Nucleoside Antimetabolite/AnalogAutophagyApoptosisnucleosideanalogueribonucleotide reductaseInhibitorinhibitorinhibit

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Clofarabine (Synonyms: 氯法拉濱)

Customer Review

Other Forms of Clofarabine:

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)