Clofarabine

Name: Clofarabine
Brand: MedChemExpress
SKU: HY-A0005
Rating: 5.0 (5 reviews)

Cat. No.: HY-A0005 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Clofarabine Chemical Structure

CAS No. : 123318-82-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 80	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 80	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 47	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 73	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 182	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Clofarabine

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

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]

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].

MedChemExpress (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.

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].

MedChemExpress (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

Molecular Weight

303.68

Formula

C₁₀H₁₁ClFN₅O₃

CAS No.

123318-82-1

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H](F)[C@H](N(C=N2)C3=C2C(N)=NC(Cl)=N3)O[C@@H]1CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (164.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (280 KB) SDS (420 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Clofarabine Related Classifications

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:

Clofarabine123318-82-1Nucleoside Antimetabolite/AnalogAutophagyApoptosisnucleosideanalogueribonucleotide reductaseInhibitorinhibitorinhibit

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Clofarabine

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Complete Stock Solution Preparation Table

Clofarabine Related Classifications

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