1. Cell Cycle/DNA Damage Apoptosis
  2. Nucleoside Antimetabolite/Analog Apoptosis
  3. Forodesine hydrochloride

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

Cat. No.: HY-16209 Purity: 98.40%
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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.

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

CAS No. : 284490-13-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Forodesine hydrochloride:

Top Publications Citing Use of Products

    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.

    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.

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

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2].

    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
    Molecular Weight

    302.71

    Formula

    C11H15ClN4O4

    CAS No.
    Appearance

    Solid

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

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

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3034 mL 16.5172 mL 33.0345 mL
    5 mM 0.6607 mL 3.3034 mL 6.6069 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    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:  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

    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

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: 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).
    Purity & Documentation

    Purity: 99.86%

    References

    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, 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.

    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.

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    • 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.

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    Product Name:
    Forodesine hydrochloride
    Cat. No.:
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