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Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $1,670 | 7-10 days |
Description | Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP. |
Targets&IC50 | PNP (human):1.19 nM , PNP (monkey):0.66 nM , PNP (mouse):0.48 nM , PNP (rat):1.24 nM , PNP (dog):1.57 nM |
In vitro | 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).Forodesine (10-30?μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation. 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%. |
In vivo | In the hu-PBL-SCID mouse model, Forodesine (BCX-1777) demonstrates efficacy in extending lifespan by two-fold or greater. This compound exhibits outstanding oral bioavailability (63%) in mice. When administered at a single dose of 10 mg/kg, it significantly increases dGuo levels to around 5 μM. |
Alias | Immucillin-H hydrochloride, BCX-1777 hydrochloride |
Molecular Weight | 302.71 |
Formula | C11H15ClN4O4 |
Cas No. | 284490-13-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 16.67 mg/mL (55.07 mM), Sonication is recommended. H2O: 16.67 mg/mL (55.07 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO/H2O
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