Fludarabine phosphate (Synonyms: NSC 118218 phosphate)

Name: Fludarabine phosphate
Brand: MedChemExpress
SKU: HY-B0028
Rating: 5.0 (4 reviews)

Cat. No.: HY-B0028 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Fludarabine phosphate Chemical Structure

CAS No. : 75607-67-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 4 publication(s) in Google Scholar

Other Forms of Fludarabine phosphate:

Fludarabine In-stock
Fludarabine triphosphate Get quote
Fludarabine phosphate (Standard) Get quote

4 Publications Citing Use of MCE Fludarabine phosphate

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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
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]
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	0.4 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]
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

Molecular Weight

365.21

Formula

C₁₀H₁₃FN₅O₇P

CAS No.

75607-67-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
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: 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 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.

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

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: 99.77%

Select Batch:

Data Sheet (281 KB) SDS (418 KB)

COA (252 KB) RP-HPLC (116 KB) MS (133 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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.

Fludarabine phosphate 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:

Fludarabine75607-67-9NSC 118218NSC118218NSC-118218Nucleoside Antimetabolite/AnalogApoptosisInhibitorinhibitorinhibit

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Fludarabine phosphate (Synonyms: NSC 118218 phosphate)

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Other Forms of Fludarabine phosphate:

Fludarabine phosphate Related Antibodies

4 Publications Citing Use of MCE Fludarabine phosphate

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Fludarabine phosphate Related Antibodies

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Complete Stock Solution Preparation Table

Fludarabine phosphate Related Classifications

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