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Forodesine
CAS No. 209799-67-7
Forodesine ( —— )
产品货号. M33362 CAS No. 209799-67-7
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)。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥561 | 有现货 |
|
| 5MG | ￥947 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称Forodesine
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注意事项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
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产品简述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)。
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产品描述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.
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体外实验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.
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体内实验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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同义词——
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通路Apoptosis
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靶点Apoptosis
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受体Apoptosis
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研究领域——
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适应症——
化学信息
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CAS Number209799-67-7
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分子量266.25
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分子式C11H14N4O4
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO 中的溶解度 : 100 mg/mL (375.59 mM; 超声助溶 )
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SMILESOC[C@H]1N[C@H]([C@H](O)[C@@H]1O)c1c[nH]c2c1nc[nH]c2=O
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895.?
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