Referencia número: HY-A0005

Clofarabine

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

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.

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Pureza: 99.83%
No. CAS: 123318-82-1
Fòrmula: C₁₀H₁₁ClFN₅O₃
Peso molecular:303.68

Almacenamiento:

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

Clofarabine Chemical Structure

No. CAS: 123318-82-1

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (15)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

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	Cytotoxicity against human BT549 cells after 5 days by SRB assay Cytotoxicity against human BT549 cells after 5 days by SRB assay	[PMID: 19929004]
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]
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]
CCRF-CEM	IC₅₀	0.05 μM Compound: Table I Row 6	Compound was tested for cytotoxicity against CCRF-CEM cell lines Compound was tested for cytotoxicity against CCRF-CEM cell lines	[PMID: 1732556]
CCRF-CEM	IC₅₀	0.06 μM Compound: 468	Anticancer activity against human CCRF-CEM cells Anticancer activity against human CCRF-CEM cells	[PMID: 34213340]
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	Cytotoxicity against human HCT15 cells after 5 days by SRB assay Cytotoxicity against human HCT15 cells after 5 days by SRB assay	[PMID: 19929004]
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]
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]
HEp-2	IC₅₀	0.012 μM Compound: 468	Anticancer activity against human HEp-2 cells Anticancer activity against human HEp-2 cells	[PMID: 34213340]
HEp-2	IC₅₀	0.012 μM Compound: Table I Row 6	Compound was tested for cytotoxicity against HEp-2 cell lines Compound was tested for cytotoxicity against HEp-2 cell lines	[PMID: 1732556]
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]
K562	IC₅₀	0.003 μM Compound: 468	Anticancer activity against human K562 cells Anticancer activity against human K562 cells	[PMID: 34213340]
K562	IC₅₀	0.003 μM Compound: Table I Row 6	Compound was tested for cytotoxicity against K562 cell lines Compound was tested for cytotoxicity against K562 cell lines	[PMID: 1732556]
L1210	IC₅₀	0.23 μM Compound: 468	Anticancer activity against mouse L1210 cells Anticancer activity against mouse L1210 cells	[PMID: 34213340]
L1210	IC₅₀	0.23 μM Compound: Table I Row 6	Compound was tested for cytotoxicity against L1210 cell lines Compound was tested for cytotoxicity against L1210 cell lines	[PMID: 1732556]
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	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]
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]
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]
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]
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]
SAOS-2	IC₅₀	>=50 μM Compound: CLF; 1	Cytotoxicity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
TC-32	IC₅₀	0.13 μM Compound: CLF; 1	Cytotoxicity against human TC-32 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human TC-32 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
U2OS	IC₅₀	>=50 μM Compound: CLF; 1	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 123318-82-1
Appearance Solid
Peso molecular 303.68
Fòrmula C₁₀H₁₁ClFN₅O₃
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (15)

All Cell Proliferation/Viability AssayApoptosis AnalysisCell Imaging/StainingIn Vivo Efficacy StudyWB

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nat Metab

Uridine-sensitized screening identifies demethoxy-coenzyme Q and NUDT5 as regulators of nucleotide synthesis. [Abstract]

2025 Nov 13. PMID: 41233602
J Immunother Cancer

Clofarabine induces tumor cell apoptosis, GSDME-related pyroptosis, and CD8+ T-cell antitumor activity via the non-canonical P53/STING pathway. [Abstract]

2025 Feb 6;13(2):e010252. PMID: 39915005

Clofarabine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Feb 6;13(2):e010252. [Abstract]

The cell viability of A375, A549, and PIG1 treated with Clofarabine (Clo) (1.25, 2.5, 5, 10, 20 μM) for 24 hours and 48 hours was measured by CCK8 assay.

Clofarabine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Feb 6;13(2):e010252. [Abstract]

Flow cytometry was conducted to determine the apoptosis of A375 and A549 treated with Clofarabine (Clo) (30 nM, 60 nM, 1 μM, 1.5 μM) for 48 hours.

Clofarabine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Feb 6;13(2):e010252. [Abstract]

The number of colonies of A375 and A549 treated with Clofarabine (Clo) for 48 hours was measured after crystal violet staining.

Clofarabine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Feb 6;13(2):e010252. [Abstract]

Schematic diagram of Clofarabine (Clo) (30 mg/kg, i.g.) for melanoma treatment. Tumor growth and body weight curves for B16F10 tumor-bearing mice receiving the designated treatments.

Clofarabine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Feb 6;13(2):e010252. [Abstract]

Western blotting revealed the protein expression of P53, p-P53, cGAS, STING, p-IkBα, BAX, Cleaved Caspase-3, Cleaved Caspase-6, and Cleaved PARP in lysates collected from A375 and A549 treated with Clofarabine (Clo).
Cell Death Dis

RRM1 inhibition sensitizes lung adenocarcinoma to decitabine treatment. [Abstract]

2026 Feb 26;17(1):275. PMID: 41748545
Acta Pharmacol Sin

Esflurbiprofen exerts a fast-onset antidepressant effect by blocking SERT-nNOS interaction. [Abstract]

2025 Oct 9. PMID: 41068287
Cell Rep

Dual inhibition of FACT and RRM2 suppresses the progression of pancreatic ductal adenocarcinoma driven by the oncohistone H2BG53D. [Abstract]

2025 Nov 23;44(12):116596. PMID: 41284383
Biochem Pharmacol

Dual inhibition of EGR1/STAT3 transcriptional hubs suppresses macrophage-driven liver fibrosis: A multi-omics-guided drug repurposing strategy. [Abstract]

2025 Oct:240:117120. PMID: 40623460
Pharmaceuticals (Basel)

Identification of Key Immune and Cell Cycle Modules and Prognostic Genes for Glioma Patients through Transcriptome Analysis. [Abstract]

2024 Sep 28;17(10):1295. PMID: 39458936
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Front Oncol

Hypoxanthine in the microenvironment can enable thiopurine resistance in acute lymphoblastic leukemia. [Abstract]

2024 Jul 19:14:1440650. PMID: 39099696
Biochem Biophys Res Commun

Connectivity-map unveils Gemcitabine's efficacy in overcoming nelarabine resistance in T-cell acute lymphoblastic leukemia. [Abstract]

2025 May 8:769:151971. PMID: 40354678
bioRxiv

Uridine-sensitized screening identifies genes and metabolic regulators of nucleotide synthesis. [Abstract]

2025 Mar 13:2025.03.11.642569. PMID: 40161720
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841

Solvente y solubilidad

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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:

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

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

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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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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RP-HPLC (2659 KB)
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OR (2659 KB)
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Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Clofarabine

15 Cited Publications

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Clofarabine

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Publications Citing Use of MedChemExpress (MCE) Clofarabine

Actividad biológica

Chemical Information

Publications (15)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Clofarabine Related Classifications

Referencia número: HY-A0005