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CAS No. : 209799-67-7
MCE 国际站:Forodesine
产品活性: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)。
研究领域:Cell Cycle/DNA Damage | Apoptosis
作用靶点:Nucleoside Antimetabolite/Analog | Apoptosis
In Vitro: 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).
In Vivo: 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.
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货号: HY-16210
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