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

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Forodesine hydrochloride (Synonyms: BCX-1777 hydrochloride; Immucillin-H hydrochloride) 纯度: 99.36%

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 PNP 的 IC50 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)。

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

Forodesine hydrochloride Chemical Structure

CAS No. : 284490-13-7

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1 mg ￥550 In-stock
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
25 mg ￥2800 In-stock
50 mg ￥5100 In-stock
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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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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

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 mg 5 mg 10 mg
1 mM 3.3035 mL 16.5175 mL 33.0349 mL
5 mM 0.6607 mL 3.3035 mL 6.6070 mL
10 mM 0.3303 mL 1.6517 mL 3.3035 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in saline)

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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

    [2]. Bantia S, et al. Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)–a novel potent and orally active immunosuppressive agent. Int Immunopharmacol. 2001 Jun;1(6):1199-210.

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