Gemcitabine(Synonyms: 吉西他滨; LY 188011)

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Gemcitabine (Synonyms: 吉西他滨; LY 188011) 纯度: 99.33%

Gemcitabine (LY 188011) 是一种嘧啶核苷类似物抗代谢药 (nucleoside antimetabolite/analog) 和抗肿瘤剂。Gemcitabine 抑制 DNA 合成 (DNA synthesis) 和修复，导致细胞自噬 (autophagy) 和凋亡 (apoptosis)。

Gemcitabine(Synonyms: 吉西他滨; LY 188011)

Gemcitabine Chemical Structure

CAS No. : 95058-81-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥792 In-stock
100 mg ￥720 In-stock
200 mg ￥1080 In-stock
500 mg ￥1980 In-stock
1 g ￥3100 In-stock
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10 g   询价  

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Gemcitabine 相关产品

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生物活性

Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis[1][2].

IC50 & Target

DNA synthesis[1]
体外研究
(In Vitro)

Gemcitabine (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4].
Gemcitabine inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, 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.

Cell Viability Assay[4]

Cell Line: Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs)
Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 3 days
Result: Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability.

体内研究
(In Vivo)

Gemcitabine can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg[2].
Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively)[3].

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

263.20

Formula

C9H11F2N3O4
CAS 号

95058-81-4
中文名称

吉西他滨；双氟脱氧胞苷
运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (949.85 mM; Need ultrasonic)

Ethanol : 12.5 mg/mL (47.49 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7994 mL 18.9970 mL 37.9939 mL
5 mM 0.7599 mL 3.7994 mL 7.5988 mL
10 mM 0.3799 mL 1.8997 mL 3.7994 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 (protect from light)。-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： 0.5%HPMC  1%Tween80

    Solubility: 20 mg/mL (75.99 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: ≥ 2.62 mg/mL (9.95 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.62 mg/mL (9.95 mM); Clear solution

  • 4.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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

  • 5.

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

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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
  • 6.

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

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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
  • 7.

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

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.90 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 8.

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

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.90 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 20.8 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]. Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80.

    [2]. Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206

    [3]. Yip-Schneider MT, et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.

    [4]. Yusheng Cai, et al. Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice. Cell Res. 2020 Jul;30(7):574-589.

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