产品描述
Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels. Forodesine hydrochloride (BCX-1777 hydrochloride) 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.
体外活性
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 values0.1-0.38 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%.
体内活性
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.Forodesine (BCX-1777) has excellent oral bioavailability (63%) in mice.?At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM.
Cas No.
284490-13-7
分子式
C11H15ClN4O4
分子量
302.71
别名
Immucillin-H hydrochloride;BCX-1777 hydrochloride;Forodesine hydrochloride
储存和溶解度
H2O:16.67 mg/mL (55.07 mM),Need ultrasonic
DMSO:16.67 mg/mL (55.07 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years