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编 号:F262366
分子式:C11H14N4O4
分子量:266.25
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
Forodesine (BCX-1777) 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. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.

体内研究:
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.

体外研究:
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 Forodesine 相关抗体:Cell Proliferation AssayCell Line:Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM)
Concentration:10?μM, 20?μM, 30?μM
Incubation Time:24 and 48 hours
Result:At the effects at 48 hours, a complete block in proliferation in the MOLT-4 cells and 15% reduction in the 5T33MM cells.
Apoptosis AnalysisCell Line:Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM)
Concentration:10?μM, 20?μM, 30?μM
Incubation Time:24 and 48 hours
Result:A limited induction of apoptosis.
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