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

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

Cat. No.: HY-16210 Purity: 99.62%
Handling Instructions Technical Support

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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CAS No. : 209799-67-7

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 19 publication(s) in Google Scholar

Other Forms of Forodesine:

Top Publications Citing Use of Products

    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.

    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.

    Forodesine 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

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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[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
    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.

    분자량

    266.25

    화학식

    C11H14N4O4

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    선적

    Room temperature in continental US; may vary elsewhere.

    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    용액&용해도
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7559 mL 18.7793 mL 37.5587 mL
    5 mM 0.7512 mL 3.7559 mL 7.5117 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.

    • 몰농도 계산기

    • 농도 희석 계산기

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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:  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.

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

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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).
    순도&문서

    Purity: 99.62%

    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, 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
    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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    • 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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    상품명:
    Forodesine
    Cat. No.:
    HY-16210
    수량:
    MCE Japan Authorized Agent: