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

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

Cat. No.: HY-16210
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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.

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

Forodesine Chemical Structure

Forodesine Chemical Structure

CAS No. : 209799-67-7

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Description

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]

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].

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].

Clinical Trial
Molecular Weight

266.25

Formula

C₁₁H₁₄N₄O₄

CAS No.

209799-67-7

SMILES
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ForodesineBCX-1777Immucillin-HBCX1777BCX 1777Nucleoside Antimetabolite/AnalogApoptosisInhibitorinhibitorinhibit

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