Art. -Nr.: HY-16209

Forodesine hydrochloride

(Synonyms: BCX-1777 hydrochloride; Immucillin-H hydrochloride)

20 Cited Publications

Kundenbewertung

Based on 20 publication(s) in Google Scholar

Forodesine hydrochloride (BCX-1777 hydrochloride) 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 hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.

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Reinheit: 98.40%
CAS. Nr.: 284490-13-7
Formel: C₁₁H₁₅ClN₄O₄
Molecular Weight:302.71

Speicherung:

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture)

Forodesine hydrochloride Chemical Structure

CAS. Nr.: 284490-13-7

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
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
PBMC	IC₅₀	<0.1 μM Compound: Forodesine Hydrochloride	Cytotoxicity against PHA stimulated human PBMC cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Cytotoxicity against PHA stimulated human PBMC cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 37801827]

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.

Clinical Trial

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

Chemical Information

CAS. Nr. 284490-13-7
Appearance Solid
Molecular Weight 302.71
Formel C₁₁H₁₅ClN₄O₄
Color Light yellow to brown
SMILES

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

BCX-1777 hydrochloride; Immucillin-H hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture)

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 hydrochloride 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 hydrochloride 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 hydrochloride 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.
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
Neurochem Res

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

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

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

2026 Jan 12:ioag007. PMID: 41524735

Forodesine hydrochloride 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 hydrochloride 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:

H₂O : 100 mg/mL (330.34 mM; Need ultrasonic)

DMSO : 10 mg/mL (33.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

3.3034 mL

16.5172 mL

33.0345 mL

5 mM

0.6607 mL

3.3034 mL

6.6069 mL

10 mM

0.3303 mL

1.6517 mL

3.3034 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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution

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: 36.67 mg/mL (121.14 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.

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 (283 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	3.3034 mL	16.5172 mL	33.0345 mL	82.5861 mL
	5 mM	0.6607 mL	3.3034 mL	6.6069 mL	16.5172 mL
	10 mM	0.3303 mL	1.6517 mL	3.3034 mL	8.2586 mL
	15 mM	0.2202 mL	1.1011 mL	2.2023 mL	5.5057 mL
	20 mM	0.1652 mL	0.8259 mL	1.6517 mL	4.1293 mL
	25 mM	0.1321 mL	0.6607 mL	1.3214 mL	3.3034 mL
	30 mM	0.1101 mL	0.5506 mL	1.1011 mL	2.7529 mL
H₂O	40 mM	0.0826 mL	0.4129 mL	0.8259 mL	2.0647 mL
	50 mM	0.0661 mL	0.3303 mL	0.6607 mL	1.6517 mL
	60 mM	0.0551 mL	0.2753 mL	0.5506 mL	1.3764 mL
	80 mM	0.0413 mL	0.2065 mL	0.4129 mL	1.0323 mL
	100 mM	0.0330 mL	0.1652 mL	0.3303 mL	0.8259 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

Forodesine hydrochloride

20 Cited Publications

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Forodesine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Forodesine hydrochloride

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Forodesine hydrochloride

Anti-Infection Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Heterocyclic Compound Library

Off-patent Drug Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Forodesine hydrochloride

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Forodesine hydrochloride Related Classifications

HY-16209 Related Classifications