1. Cell Cycle/DNA Damage Apoptosis
  2. Nucleoside Antimetabolite/Analog Apoptosis
  3. Forodesine hydrochloride

Forodesine hydrochloride  (Synonyms: BCX-1777 hydrochloride; Immucillin-H hydrochloride)

目录号: HY-16209 纯度: 99.34%
COA 产品使用指南

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)。

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Forodesine hydrochloride Chemical Structure

Forodesine hydrochloride Chemical Structure

CAS No. : 284490-13-7

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Other Forms of Forodesine hydrochloride:

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Forodesine hydrochloride (BCX-1777 hydrochloride) 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 hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

302.71

Formula

C11H15ClN4O4

CAS 号
性状

固体

颜色

Light brown to brown

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, 1 year; -20°C, 6 months (stored under nitrogen)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 100 mg/mL (330.34 mM; 超声助溶)

DMSO 中的溶解度 : 10 mg/mL (33.03 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3034 mL 16.5172 mL 33.0345 mL
5 mM 0.6607 mL 3.3034 mL 6.6069 mL
查看完整储备液配制表

* 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°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    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); 澄清溶液

  • 方案 二

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.65 mM); 澄清溶液

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 36.67 mg/mL (121.14 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.86%

参考文献

完整储备液配制表

* 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°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.3034 mL 16.5172 mL 33.0345 mL 82.5861 mL
5 mM 0.6607 mL 3.3034 mL 6.6069 mL 16.5172 mL
10 mM 0.3303 mL 1.6517 mL 3.3034 mL 8.2586 mL
15 mM 0.2202 mL 1.1011 mL 2.2023 mL 5.5057 mL
20 mM 0.1652 mL 0.8259 mL 1.6517 mL 4.1293 mL
25 mM 0.1321 mL 0.6607 mL 1.3214 mL 3.3034 mL
30 mM 0.1101 mL 0.5506 mL 1.1011 mL 2.7529 mL
H2O 40 mM 0.0826 mL 0.4129 mL 0.8259 mL 2.0647 mL
50 mM 0.0661 mL 0.3303 mL 0.6607 mL 1.6517 mL
60 mM 0.0551 mL 0.2753 mL 0.5506 mL 1.3764 mL
80 mM 0.0413 mL 0.2065 mL 0.4129 mL 1.0323 mL
100 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8259 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Forodesine hydrochloride
目录号:
HY-16209
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