Tezacitabine(Synonyms: 替扎西他滨)

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Tezacitabine (Synonyms: 替扎西他滨) 纯度: 99.32%

Tezacitabine 是一种具有细胞生长抑制和细胞毒性的抗代谢药，是一种核苷类似物。Tezacitabine 不可逆地抑制核糖核苷酸还原酶 (ribonucleotide reductase) 并干扰 DNA 复制和修复。Tezacitabine 有效诱导细胞凋亡 (apoptotic)，可用于白血病和实体瘤的研究。

Tezacitabine(Synonyms: 替扎西他滨)

Tezacitabine Chemical Structure

CAS No. : 130306-02-4

规格 价格 是否有货 数量
5 mg ￥9700 In-stock
10 mg ￥15500 In-stock
50 mg   询价  
100 mg   询价  

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Tezacitabine 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment[1][2].

IC50 & Target

Ribonucleotide reductase[1]
体外研究
(In Vitro)

Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment induces the G1 and S-phase leaky block of the cell cycle[1].
Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner[1].
Tezacitabine has strong cytostatic and cytotoxic properties. Cytotoxic effect of Tezacitabine reveals not only as apoptosis, but also as a change in protein metabolism[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
Incubation Time: 24 hours
Result: Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle.

Apoptosis Analysis[1]

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
Incubation Time: 24 hours
Result: Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.

体内研究
(In Vivo)

Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (7-9-week-old) injected with HCT 116 cells[2]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; daily; 14 days
Result: Inhibited tumor growth in HCT 116 tumor xenografts.

Clinical Trial

分子量

257.22

Formula

C10H12FN3O4
CAS 号

130306-02-4
中文名称

替扎西他滨
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-80°C
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (777.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8877 mL 19.4386 mL 38.8772 mL
5 mM 0.7775 mL 3.8877 mL 7.7754 mL
10 mM 0.3888 mL 1.9439 mL 3.8877 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。-80°C 储存时，请在 6 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: ≥ 5 mg/mL (19.44 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (19.44 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (19.44 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (19.44 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (19.44 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (19.44 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 50.0 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Janusz S Skierski, et al. Tezacitabine Blocks Tumor Cells in G1 and S Phases of the Cell Cycle and Induces Apoptotic Cell Death. Acta Pol Pharm. May-Jun 2005;62(3):195-205.

    [2]. Pietro Taverna, et al. Tezacitabine Enhances the DNA-directed Effects of Fluoropyrimidines in Human Colon Cancer Cells and Tumor Xenografts. Biochem Pharmacol. 2007 Jan 1;73(1):44-55.

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