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Forodesine hydrochloride
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 hydrochloride图片
CAS NO:284490-13-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
BCX-1777 hydrochloride
Immucillin-H hydrochloride
产品介绍
Forodesine hydrochloride (BCX-1777 hydrochloride) 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 hydrochloride 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 hydrochloride (BCX-1777 hydrochloride) 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 hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride 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) (IC50values< 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

302.71

性状

Solid

Formula

C11H15ClN4O4

CAS 号

284490-13-7

中文名称

呋咯地辛盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

H2O : 100 mg/mL(330.35 mM;Need ultrasonic)

DMSO : 10 mg/mL(33.03 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.3035 mL16.5175 mL33.0349 mL
5 mM0.6607 mL3.3035 mL6.6070 mL
10 mM0.3303 mL1.6517 mL3.3035 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 36.67 mg/mL (121.14 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution

*以上所有助溶剂都可在本网站选购。