Fluorizoline

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Fluorizoline  纯度: 99.77%

Fluorizoline 选择性地直接结合到 prohibitin 1 (PHB1) 和 2 (PHB2),并诱导凋亡。Fluorizoline 通过上调 NOXA 和 BIM 降低慢性淋巴细胞性白血病 (CLL) 细胞的活力。Fluorizoline 以 p53 非依赖性方式发挥抗肿瘤作用。

Fluorizoline

Fluorizoline Chemical Structure

CAS No. : 1362243-70-6

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10 mM * 1 mL in DMSO ¥990 In-stock
5 mg ¥900 In-stock
10 mg ¥1700 In-stock
25 mg ¥3500 In-stock
50 mg ¥5500 In-stock
100 mg ¥9500 In-stock
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Fluorizoline 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

Fluorizoline selectively and directly binds to prohibitin 1 (PHB1) and 2 (PHB2), and induces apoptosis. Fluorizoline reduces chronic lymphocytic leukemia (CLL) cell viability through the upregulation of NOXA and BIM. Fluorizoline exerts antitumor action in a p53-independent manner[1].

体外研究
(In Vitro)

Fluorizoline (1.25-20 μM; 24 hours) induces apoptosis in primary CLL cells ex vivo[1].
Fluorizoline (5-10 μM; 48 hours) causes an increase of NOXA protein levels[1].
Fluorizoline reduces the percentage of viable normal B and T cells (48.6% and 82.8% of viable cells at 24 hours of treatment with 10 μM Fluorizoline in normal CD19+ and CD3+ populations, respectively) with mean EC50 values of 10.9 μM and 19.1 μM at 24 hours for normal B and T cells, respectively[1].

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.

Apoptosis Analysis[1]

Cell Line: Primary CLL cells
Concentration: 1.25 to 20 μM
Incubation Time: 24 hours
Result: Strongly reduced cell viability and induced apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Primary CLL cells
Concentration: 5, 10 μM
Incubation Time: 48 hours
Result: Caused an increase of NOXA protein levels.

体内研究
(In Vivo)

Fluorizoline (15 mg/kg; ip; three times a week for five weeks) becomes very rapidly (3 weeks) leukemic, as reflected by the increase in the percentage and the number of CD5+CD19+ CLL cells in the blood in 6-week-old recipient C57BL/6 Eμ-TCL1 mouse model of CLL. Fluorizoline does not induce apoptosis in vivo. Fluorizoline does not control disease development in the spleen as indicated by enlarged spleens[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.

分子量

362.20

Formula

C15H8Cl2F3NS

CAS 号

1362243-70-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (138.05 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7609 mL 13.8045 mL 27.6091 mL
5 mM 0.5522 mL 2.7609 mL 5.5218 mL
10 mM 0.2761 mL 1.3805 mL 2.7609 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。-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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.90 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.90 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*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]. Ana M Cosialls, et al. The prohibitin-binding compound fluorizoline induces apoptosis in chronic lymphocytic leukemia cells through the upregulation of NOXA and synergizes with ibrutinib, 5-aminoimidazole-4-carboxamide riboside or venetoclax. Haematologica. 2017 Sep;102(9):1587-1593.

    [2]. Marina Wierz, et al. The prohibitin-binding compound fluorizoline induces apoptosis in chronic lymphocytic leukemia cells ex vivo but fails to prevent leukemia development in a murine model. Haematologica. 2018 Apr;103(4):e154-e157.

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