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Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.
Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 12,980 | 10-14周 | |
100 mg | 询价 | 10-14周 |
产品描述 | Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP. |
靶点活性 | PNP (human):1.19 nM , PNP (monkey):0.66 nM , PNP (mouse):0.48 nM , PNP (rat):1.24 nM , PNP (dog):1.57 nM |
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 values 0.1-0.38 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. |
别名 | Immucillin-H hydrochloride, BCX-1777 hydrochloride |
分子量 | 302.71 |
分子式 | C11H15ClN4O4 |
CAS No. | 284490-13-7 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 16.67 mg/mL (55.07 mM), Sonication is recommended. H2O: 16.67 mg/mL (55.07 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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