Art. -Nr.: HY-B0028

Fludarabine phosphate

(Synonyms: NSC 118218 phosphate)

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

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

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Reinheit: 99.77%
CAS. Nr.: 75607-67-9
Formel: C₁₀H₁₃FN₅O₇P
Molecular Weight:365.21

Speicherung:

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

Fludarabine phosphate Chemical Structure

CAS. Nr.: 75607-67-9

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.4 μM Compound: 466	Anticancer activity against human CCRF-CEM cells Anticancer activity against human CCRF-CEM cells	[PMID: 34213340]
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]
HEp-2	IC₅₀	9 μM Compound: 466	Anticancer activity against human HEp-2 cells Anticancer activity against human HEp-2 cells	[PMID: 34213340]
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	0.15 μM Compound: 466	Anticancer activity against human K562 cells Anticancer activity against human K562 cells	[PMID: 34213340]
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]
L1210	IC₅₀	3 μM Compound: 466	Anticancer activity against mouse L1210 cells Anticancer activity against mouse L1210 cells	[PMID: 34213340]
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]

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].

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

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].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 75607-67-9
Appearance Solid
Molecular Weight 365.21
Formel C₁₀H₁₃FN₅O₇P
Color White to off-white
SMILES

NC1=C2C(N([C@H]3[C@@H](O)[C@H](O)[C@@H](COP(O)(O)=O)O3)C=N2)=NC(F)=N1
Synonyms

NSC 118218 phosphate
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (9)

All Cell Proliferation/Viability AssayWBFlow CytometryIn Vivo Efficacy Study

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Journal Impact Factor

Nat Cancer

Different niches for stem cells carrying the same oncogenic driver affect pathogenesis and therapy response in myeloproliferative neoplasms. [Abstract]

2023 Aug;4(8):1193-1209. PMID: 37550517
Nat Metab

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

2025 Nov 13. PMID: 41233602
Cell Stem Cell

MMRN1-EGFR drives sialylglycan-Siglec immune evasion in AML leukemia stem cells. [Abstract]

2026 May 7;33(5):800-819.e9. PMID: 42030946
Nat Cell Biol

NAT10-mediated mRNA N4-acetylcytidine reprograms serine metabolism to drive leukaemogenesis and stemness in acute myeloid leukaemia. [Abstract]

2024 Dec;26(12):2168-2182. PMID: 39506072

Fludarabine phosphate purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Dec;26(12):2168-2182. [Abstract]

MTT assays and the IC50 values of Remodelin, Fludarabine, fosaprepitant, dantrolene and folinic acid in MOLM13 cells after 72 h of treatment.

Fludarabine phosphate purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Dec;26(12):2168-2182. [Abstract]

Western blotting showing the protein levels of NAT10 targets and downstream genes in MOLM13 cells with Fludarabine or Remodelin treatment.

Fludarabine phosphate purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Dec;26(12):2168-2182. [Abstract]

The proportion of MOLM13 cells at different cell cycle stages after treatment with 20 μM Remodelin or 1 μM Fludarabine for 72 hours. Examples show EdU labeling and PI staining, followed by flow cytometry assessment of the MOLM13 cell cycle.

Fludarabine phosphate purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Dec;26(12):2168-2182. [Abstract]

Body weight of C1498 homologous AML mice after intraperitoneal injection of Fludarabine (200 mg/kg) or corresponding vector control.
J Mol Med (Berl)

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

2019 Aug;97(8):1183-1193. PMID: 31201471
Antiviral Res

Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. [Abstract]

2020 Jun;178:104786. PMID: 32251767
Carcinogenesis

A2AR-phospho-STAT1 (Y701)-HLA-E axis as a potential immune modulatory pathway in radiotherapy-resistant triple negative breast cancer. [Abstract]

2025 Oct 22:bgaf069. PMID: 41122851
bioRxiv

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

2025 Mar 13:2025.03.11.642569. PMID: 40161720
Research Square Print

2022 Aug.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (273.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (13.69 mM; Need ultrasonic)

* "≥" 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

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

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: phosphate buffer Saline

Solubility: 20 mg/mL (54.76 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 18.33 mg/mL (50.19 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Protokoll

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.

MedChemExpress (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).

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (419 KB)
- English - EN (419 KB)
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- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
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- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Fludarabine phosphate

9 Cited Publications

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Fludarabine phosphate

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Publications Citing Use of MedChemExpress (MCE) Fludarabine phosphate

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fludarabine phosphate Related Classifications

HY-B0028 Related Classifications