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Chemical Structure| 209799-67-7 Chemical Structure| 209799-67-7

Structure of Forodesine
CAS No.: 209799-67-7

Chemical Structure| 209799-67-7

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Forodesine (BCX-1777) is a potent, 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.

Synonyms: BCX-1777; Immucillin-H

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Product Details of Forodesine

CAS No. :209799-67-7
Formula : C11H14N4O4
M.W : 266.25
SMILES Code : O=C1C(NC=C2[C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O)=C2N=CN1
Synonyms :
BCX-1777; Immucillin-H
MDL No. :MFCD09837827

Safety of Forodesine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Forodesine

epigenetics
DNA

Isoform Comparison

Biological Activity

Description
Forodesine (BCX-1777) is identified as a potent, orally active inhibitor of purine nucleoside phosphorylase (PNP), showing IC50 values ranging from 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP. It notably hinders human lymphocyte proliferation and induces apoptosis in leukemic cells by elevating dGTP levels[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 2 μM 24 h inhibition of PNP activity, attenuation of HeLa cell growth Nat Metab. 2020 Jul;2(7):635-647
human peripheral blood mononuclear cells (PBMCs) 2 μM 24 h inhibition of PNP activity, attenuation of bioenergetic activity in Teff cells Nat Metab. 2020 Jul;2(7):635-647
renal microvascular smooth muscle cells 10 μmol/L 30 minutes To evaluate the effects of Forodesine on 3',5'-cAMP and inosine levels. In WT cells, Forodesine increased 3',5'-cAMP and inosine levels; in A2B-KO cells, only inosine levels were increased. Hypertension. 2023 May;80(5):981-994
PBMCs 10 μM 72 hours Evaluate the cytotoxicity of Forodesine on primary peripheral blood mononuclear cells J Med Chem. 2023 May 25;66(10):6652-6681

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Sprague-Dawley rats Intravenous injection 2 mg/kg Single dose Forodesine reduced the metabolism of 8-nitroguanosine via pathway 2 and shunted the metabolism of 8-nitroguanosine to 8-aminoguanosine. Biochem Pharmacol. 2022 Jul;201:115076

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00742495 Relapsed or Refractory T-cell ... More >>Acute Lymphoblastic Leukaemia|B-cell Precursor Acute Lymphoblastic Leukaemia|T-cell Non-Hodgkin's Lymphoma Less << PHASE1|PHASE2 TERMINATED 2025-09-10 Vienna, Austria|Prague, Czech ... More >>Republic|Prof Gerard Michel, Marseilles, France|Charite Universitymedicine, Berlin, Germany|Dr Giovanna Gioriani, Pavia, Italy|Sally Kinsey, Leeds, United Kingdom Less <<
NCT00035022 Leukemia, Lymphocytic|Lymphoma PHASE1|PHASE2 COMPLETED 2025-03-04 M.D. Anderson Cancer Center, H... More >>ouston, Texas, 77030, United States Less <<
NCT00646165 B-cell Chronic Lymphocytic Leu... More >>kemia Less << PHASE1 TERMINATED 2025-05-09 H. Clinic I Provincial, Barcel... More >>ona, 08036, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.76mL

0.75mL

0.38mL

18.78mL

3.76mL

1.88mL

37.56mL

7.51mL

3.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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