Art. -Nr.: HY-16210

Forodesine

(Synonyms: BCX-1777; Immucillin-H)

20 Cited Publications

Kundenbewertung

Based on 20 publication(s) in Google Scholar

Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC₅₀ values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.

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Reinheit: 99.62%
CAS. Nr.: 209799-67-7
Formel: C₁₁H₁₄N₄O₄
Molecular Weight:266.25

Speicherung:

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

Forodesine Chemical Structure

CAS. Nr.: 209799-67-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.19 nM (Human PNP), 0.48 nM (Mouse PNP), 1.24 nM (Rat PNP), 0.66 nM (Monkey PNP) and 1.57 nM (Dog PNP)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	0.003 μM Compound: Forodesine	Cytotoxicity against human CCRF-CEM cells assessed as cell viability incubated for 72 hrs by XTT assay Cytotoxicity against human CCRF-CEM cells assessed as cell viability incubated for 72 hrs by XTT assay	[PMID: 37134237]
Jurkat	CC₅₀	0.003 μM Compound: Forodesine	Cytotoxicity against human Jurkat cells assessed as cell viability incubated for 72 hrs by XTT assay Cytotoxicity against human Jurkat cells assessed as cell viability incubated for 72 hrs by XTT assay	[PMID: 37134237]
MOLT-4	CC₅₀	0.004 μM Compound: Forodesine	Cytotoxicity against human MOLT-4 cells assessed as cell viability incubated for 72 hrs by XTT assay Cytotoxicity against human MOLT-4 cells assessed as cell viability incubated for 72 hrs by XTT assay	[PMID: 37134237]
MRC5	IC₅₀	>64 μM Compound: ImmH	Cytotoxicity against human MRC5 SV2 cells after 48 hrs Cytotoxicity against human MRC5 SV2 cells after 48 hrs	[PMID: 20194690]

In Vitro

Forodesine (10-30 μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation^[1].
Forodesine (10-30 μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) has no effect on the MM cells at 24 hours, while it could reduce the percentage of living cells in the MOLT-4 cells with 40%^[1].
Forodesine (BCX-1777), in the presence of 2'-deoxyguanosine (dGuo, 3-10 μM), inhibits human lymphocyte proliferation activated by various agents such as interleukin-2 (IL-2), mixed lymphocyte reaction (MLR) and phytohemagglutinin (PHA) (IC50 values < 0.1-0.38 μM)^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM)
Concentration:

10 μM, 20 μM, 30 μM
Incubation Time:

24 and 48 hours
Result:

At the effects at 48 hours, a complete block in proliferation in the MOLT-4 cells and 15% reduction in the 5T33MM cells.

Apoptosis Analysis^[1]

Cell Line:

Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM)
Concentration:

10 μM, 20 μM, 30 μM
Incubation Time:

24 and 48 hours
Result:

A limited induction of apoptosis.

In Vivo

Forodesine (BCX-1777) has excellent oral bioavailability (63%) in mice^[2].
At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM^[2].
n the human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model, Forodesine is effective in prolonging the life span 2-fold or more^[2].

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

Chemical Information

CAS. Nr. 209799-67-7
Appearance Solid
Molecular Weight 266.25
Formel C₁₁H₁₄N₄O₄
Color White to yellow
SMILES

O=C1C(NC=C2[C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O)=C2NC=N1
Synonyms

BCX-1777; Immucillin-H
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 (20)

All Bio/Physico-chemical AssayWBHistological Imaging/StainingCell Proliferation/Viability Assay

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Journal Impact Factor

Cell

Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior. [Abstract]

2019 Oct 31;179(4):864-879.e19. PMID: 31675497
Cell Metab

Stress triggers irritable bowel syndrome with diarrhea through a spermidine-mediated decline in type I interferon. [Abstract]

2025 Jan 7;37(1):87-103.e10. PMID: 39366386
Nat Metab

Inosine is an alternative carbon source for CD8+-T-cell function under glucose restriction. [Abstract]

2020 Jul;2(7):635-647. PMID: 32694789
Nucleic Acids Res

SPRINT: a Cas13a-based platform for detection of small molecules. [Abstract]

2020 Sep 25;48(17):e101. PMID: 32797156
Med

Large-scale quantitative metabolomics and mass spectrometry imaging define the metabolic atlas in human acute type A aortic dissection. [Abstract]

2026 Mar 27:101078. PMID: 41903544
Biosens Bioelectron

A thermophoresis-based biosensor for real-time detection of inorganic phosphate during enzymatic reactions. [Abstract]

2020 Dec 1:169:112616. PMID: 32979591
Int J Biol Sci

Xanthine dehydrogenase rewires metabolism and the survival of nutrient deprived lung adenocarcinoma cells by facilitating UPR and autophagic degradation. [Abstract]

2023 Jan 1;19(3):772-788. PMID: 36778128
Chem Sci

Enzyme-activatable charge transfer in gold nanoclusters. [Abstract]

2024 May 14;15(23):8922-8933. PMID: 38873061

Forodesine purchased from MedChemExpress. Usage Cited in: Chem Sci. 2024 May 14;15(23):8922-8933. [Abstract]

Dose-dependent inhibition of PNP activity (20 U/L) by Forodesine (1-5 μM; 60 min) using MPR-AuNCs as luminescent probes. The inset shows structure of Forodesine.
Cell Rep

SAMHD1 Limits the Efficacy of Forodesine in Leukemia by Protecting Cells against the Cytotoxicity of dGTP. [Abstract]

2020 May 12;31(6):107640. PMID: 32402273
J Med Chem

Design, Synthesis, Biological Evaluation, and Crystallographic Study of Novel Purine Nucleoside Phosphorylase Inhibitors. [Abstract]

2023 May 25;66(10):6652-6681. PMID: 37134237
Plant J

Plant nucleoside N-ribohydrolases: riboside binding and role in nitrogen storage mobilization. [Abstract]

2024 Mar;117(5):1432-1452. PMID: 38044809
Am J Physiol Cell Physiol

Adipose tissue releases nucleosides. [Abstract]

2026 Jan 1;330(1):C142-C154. PMID: 41269663
Oncol Res

PNP as a Metabolic and Prognostic Driver of Breast Cancer Aggressiveness: Insights from Patient Tissue and Cell Models. [Abstract]

2025 Dec 30;34(1):13. PMID: 41502507

Forodesine purchased from MedChemExpress. Usage Cited in: Oncol Res. 2025 Dec 30;34(1):13. [Abstract]

Correlation between PNP and HER-2 in SKBR3 cells. Western blot analysis showing protein expression levels of HER-2 and PNP in SKBR3 cells treated with vehicle control (CTL), Forodesine (BCX-1777, a PNP inhibitor; 10 μM; 48 h), or trastuzumab (a HER-2 inhibitor). The results showed that inhibition of PNP using BCX-1777 resulted in significant (p < 0.01) upregulation of HER-2 by ~1.45 fold.

Forodesine purchased from MedChemExpress. Usage Cited in: Oncol Res. 2025 Dec 30;34(1):13. [Abstract]

SKBR3 cell viability was assessed using the MTT assay and expressed as a percentage relative to untreated control (CTL) cells. Data shown are representative blots from three independent biological replicates (n = 3). The results showed that treatment with Forodesine (BCX-1777, 10 μM; 48 h) alone, a pharmacological PNP inhibitor, significantly reduced the cell viability by ~30%. A combination of BCX-1777 with trastuzumab resulted in a further reduction in the cell viability (~34%, p < 0.01). These results demonstrated that inhibition of PNP enhanced the cytotoxic effect of HER-2 inhibition.
Neurochem Res

ATP Restoration by ATP-Deprived Cultured Primary Astrocytes. [Abstract]

2024 Nov 16;50(1):13. PMID: 39549173
J Biol Chem

Entecavir competitively inhibits deoxyguanosine and deoxyadenosine phosphorylation in isolated mitochondria and the perfused rat heart. [Abstract]

2022 May;298(5):101876. PMID: 35358513
Biol Reprod

Hypoxanthine is involved in promoting the activation of mouse primordial follicles†. [Abstract]

2026 Jan 12:ioag007. PMID: 41524735

Forodesine purchased from MedChemExpress. Usage Cited in: Biol Reprod. 2026 Jan 12:ioag007. [Abstract]

The adolescent mice were administered water either with or without 0-15 mg/kg Forodesine (BCX-1777) for 1 week, and then the ovaries were obtained for immunofluorescence and hematoxylin staining. The results showed that compared with the control, oral administration of 10 and 15 mg/kg BCX-1777 significantly decreased the number of growing follicles in the ovaries.

Forodesine purchased from MedChemExpress. Usage Cited in: Biol Reprod. 2026 Jan 12:ioag007. [Abstract]

The adolescent mice were administered water either with or without 0-15 mg/kg Forodesine (BCX-1777) for 1 week, and then the ovaries were obtained for hypoxanthine concentration detection. The results showed that, compared with the control, oral administration of 10 and 15 mg/kg BCX-1777 significantly decreased hypoxanthine levels in the ovaries.
bioRxiv

2026 May 18.
Blood Immunol Cell Ther

2026 Jan 12.
SSRN

2024 Mar 14.
bioRxiv

2019 Oct.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (375.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 20 mg/mL (75.12 mM; Need ultrasonic)

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

3.7559 mL

18.7793 mL

37.5587 mL

5 mM

0.7512 mL

3.7559 mL

7.5117 mL

10 mM

0.3756 mL

1.8779 mL

3.7559 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.39 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 2

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

Solubility: ≥ 2.5 mg/mL (9.39 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 3

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

Solubility: ≥ 2.5 mg/mL (9.39 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.

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895. [Content Brief]

[2]. Bantia S, et al. Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)--a novel potent and orally active immunosuppressive agent. Int Immunopharmacol. 2001 Jun;1(6):1199-210. [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	3.7559 mL	18.7793 mL	37.5587 mL	93.8967 mL
	5 mM	0.7512 mL	3.7559 mL	7.5117 mL	18.7793 mL
	10 mM	0.3756 mL	1.8779 mL	3.7559 mL	9.3897 mL
	15 mM	0.2504 mL	1.2520 mL	2.5039 mL	6.2598 mL
	20 mM	0.1878 mL	0.9390 mL	1.8779 mL	4.6948 mL
	25 mM	0.1502 mL	0.7512 mL	1.5023 mL	3.7559 mL
	30 mM	0.1252 mL	0.6260 mL	1.2520 mL	3.1299 mL
	40 mM	0.0939 mL	0.4695 mL	0.9390 mL	2.3474 mL
	50 mM	0.0751 mL	0.3756 mL	0.7512 mL	1.8779 mL
	60 mM	0.0626 mL	0.3130 mL	0.6260 mL	1.5649 mL
DMSO	80 mM	0.0469 mL	0.2347 mL	0.4695 mL	1.1737 mL
DMSO	100 mM	0.0376 mL	0.1878 mL	0.3756 mL	0.9390 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.

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Keywords

Forodesine

20 Cited Publications

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Forodesine

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Forodesine hydrochloride

SBE-β-CD

5-Fluorouracil

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Publications Citing Use of MedChemExpress (MCE) Forodesine

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Forodesine

6-Mercaptopurine

Forodesine hydrochloride

SBE-β-CD

5-Fluorouracil

Venetoclax

Dipyridamole

Allopurinol

Gemcitabine elaidate

Azathioprine

Aminooxyacetic acid hemihydrochloride

Heparan Sulfate

Febuxostat

Publications Citing Use of MedChemExpress (MCE) Forodesine

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Forodesine Related Classifications

HY-16210 Related Classifications

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