Forodesine (BCX-1777) 是一种高效的口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂，对人，小鼠，大鼠，猴和狗 PNP 的 IC₅₀ 值在 0.48 至 1.57 nM 之间。Forodesine 是有效的人类淋巴细胞增殖抑制剂，可通过增加 dGTP 水平而诱导白血病细胞凋亡 (apoptosis)。

Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC 50 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.

Solid

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)

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%.
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). has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895.
[2]. Bantia S, et al. Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)--a novel potent and orally active immunosuppressive agent. Int Immunopharmacol. 2001 Jun;1(6):1199-210.