Forodesine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

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).Cell Proliferation Assay Cell 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 Analysis Cell 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.

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. 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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Apoptosis

Apoptosis

Apoptosis

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209799-67-7

266.25

C11H14N4O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (375.59 mM; 超声助溶 )

OC[C@H]1N[C@H]([C@H](O)[C@@H]1O)c1c[nH]c2c1nc[nH]c2=O

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(-20℃)

With Ice Pack

≥ 2 years