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Forodesine hydrochloride

CAS No. : 284490-13-7

MCE 站：Forodesine hydrochloride

产品活性：Forodesine hydrochloride (BCX-1777 hydrochloride) 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 hydrochloride 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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