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Forodesine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Forodesine图片
CAS NO:209799-67-7
包装:5mg
市场价:5500元

产品名称
呋咯地辛
BCX-1777
Immucillin-H
产品介绍
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PNPIC50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)。
生物活性

Forodesine (BCX-1777) is a highly potent and orally activepurine nucleoside phosphorylase (PNP)inhibitor withIC50values ranging from 0.48 to 1.57 nM forhuman, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induceapoptosisin leukemic cells by increasing the dGTP levels[1][2].

IC50& Target

IC50: 1.19 nM (Human PNP), 0.48 nM (Mouse PNP), 1.24 nM (Rat PNP), 0.66 nM (Monkey PNP) and 1.57 nM (Dog PNP)[2]

体外研究
(In Vitro)

Forodesine (10-30 μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation[1].
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%[1].
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)[2].

Cell Proliferation Assay[1]

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[1]

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.
体内研究
(In Vivo)

Forodesine (BCX-1777) has excellent oral bioavailability (63%) in mice[2].
At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM[2].
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[2].

Clinical Trial
分子量

266.25

性状

Solid

Formula

C11H14N4O4

CAS 号

209799-67-7

中文名称

呋咯地辛

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month