Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine is an orally active inhibitor of purine nucleoside phosphorylase (IC50s: 0.48 to 1.57 nM for human, mouse, rat, monkey, and dog PNP). It could induce apoptosis in leukemic cells by increasing the dGTP levels.

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 decrease the percentage of living cells in the MOLT-4 cells with 40%. Forodesine (10-30?μM; 24 and 48 hours; RPMI-8226, MOLT-4, and 5T33MM cells) treatment is partially inhibition of proliferation [1]. Forodesine inhibits human lymphocyte proliferation activated by various agents such as interleukin-2 (IL-2), mixed lymphocyte reaction (MLR) and phytohemagglutinin (PHA) (IC50s< 0.1-0.38 μM), in the presence of 2'-deoxyguanosine (dGuo, 3-10 μM) [2].

Forodesine has excellent oral bioavailability (63%) in mice. Forodesine(single dose of 10 mg/kg; in mice ) treatment, elevates dGuo to approximately 5 μM. Forodesine is effective in prolonging the life span 2-fold or more, in the human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model [2].

209799-67-7

C11H14N4O4

266.25

BCX-1777;Immucillin-H;呋咯地辛;Forodesine

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years