标签归档：gemcitabine

Gemcitabine-O-Si(di-iso)-O-Mc

发表于由

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。

Gemcitabine-O-Si(di-iso)-O-Mc  纯度: 95.02%

Gemcitabine-O-Si(di-iso)-O-Mc 是抗体偶联药物的一部分，由嘧啶核苷类似物抗代谢药和抗肿瘤剂 Gemcitabine (HY-17026) 和 ADC linker 连接而成。

Gemcitabine-O-Si(di-iso)-O-Mc

Gemcitabine-O-Si(di-iso)-O-Mc Chemical Structure

规格 价格 是否有货 数量
1 mg ￥5500 In-stock
5 mg ￥9800 In-stock
10 mg ￥15000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

生物活性

Gemcitabine-O-Si(di-iso)-O-Mc is a drug-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker[1].

体外研究
(In Vitro)

Antibody drug conjugates (ADC) couple therapeutic monoclonal antibodies (mAb) with potent toxins through a linker that is stable within systemic circulation, but cleaves within the target cells[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.
分子量

558.65

Formula

C24H36F2N4O7Si
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (179.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7900 mL 8.9501 mL 17.9003 mL
5 mM 0.3580 mL 1.7900 mL 3.5801 mL
10 mM 0.1790 mL 0.8950 mL 1.7900 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： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.48 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.48 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]. Mathew C. Finniss, et al. A versatile acid-labile linker for antibody–drug conjugate. MedChemComm, Issue 9, 2014.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Gemcitabine(Synonyms: 吉西他滨; LY 188011)

发表于由

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。

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
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Gemcitabine 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Natural Product Like Compound Library
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Nucleotide Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Gemcitabine hydrochloride(Synonyms: 盐酸吉西他滨; LY 188011 hydrochloride)

发表于由

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。

Gemcitabine hydrochloride (Synonyms: 盐酸吉西他滨; LY 188011 hydrochloride) 纯度: 99.87%

Gemcitabine Hydrochloride (LY 188011 Hydrochloride) 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 hydrochloride(Synonyms: 盐酸吉西他滨; LY 188011 hydrochloride)

Gemcitabine hydrochloride Chemical Structure

CAS No. : 122111-03-9

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
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Gemcitabine hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Natural Product Like Compound Library
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Nucleotide Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

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

IC50 & Target

DNA synthesis[1]
体外研究
(In Vitro)

Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4].
Gemcitabine Hydrochloride 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 Hydrochloride 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 Hydrochloride 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

299.66

Formula

C9H12ClF2N3O4
CAS 号

122111-03-9
中文名称

盐酸吉西他滨；吉西他宾盐酸盐
运输条件

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

4°C, sealed storage, away from moisture and light

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

H2O : ≥ 66.66 mg/mL (222.45 mM)

DMSO : 25 mg/mL (83.43 mM; ultrasonic and warming and heat to 60°C)

DMF : 2.5 mg/mL (8.34 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3371 mL 16.6856 mL 33.3712 mL
5 mM 0.6674 mL 3.3371 mL 6.6742 mL
10 mM 0.3337 mL 1.6686 mL 3.3371 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 (sealed storage, away from moisture and 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： PBS

    Solubility: 60 mg/mL (200.23 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.94 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.94 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
  • 4.

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

    Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.94 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]. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149.

    [4]. 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Gemcitabine elaidate hydrochloride(Synonyms: CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5′-elaidate hydrochloride)

发表于由

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。

Gemcitabine elaidate hydrochloride (Synonyms: CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5′-elaidate hydrochloride) 纯度: ≥97.0%

Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 具有抗肿瘤活性。

Gemcitabine elaidate hydrochloride(Synonyms: CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5

Gemcitabine elaidate hydrochloride Chemical Structure

规格 价格 是否有货 数量
5 mg ￥1050 In-stock
10 mg ￥1450 In-stock
50 mg ￥4450 In-stock
100 mg ￥6680 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Gemcitabine elaidate hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity[1][2].

体外研究
(In Vitro)

Gemcitabine elaidate (0.2 nM-1 mM; 72 h) hydrochloride inhibits the growth of gemcitabine sensitive and resistant cells, with IC50s of 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4 and MOLT4/C8 cells, respectively[1].
Gemcitabine elaidate (0.5 nM-1 μM; 72 h) hydrochloride increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells[2].

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

Cell Cycle Analysis[2]

Cell Line: A549 and WiDR cells
Concentration: 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM
Incubation Time: 72 h
Result: Induced a G2/M and S phase accumulation.

体内研究
(In Vivo)

Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) hydrochloride inhibits the solid tumor xenografts growth of non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), pancreatic cancer (PANC-1)[1].
Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) hydrochloride shows acceptable toxicity and significant antitumor activity in the colon cancer xenograft Co6044 bearing mice[1].
Gemcitabine elaidate (p.o. once daily for 5 doses) hydrochloride shows a favorable toxicity and antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044[1].

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

Animal Model: Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively[1]
Dosage: 25-120 mg/kg
Administration: I.p. every 3 days for 5 doses
Result: Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.

分子量

564.11

Formula

C27H44ClF2N3O5
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 : 100 mg/mL (177.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7727 mL 8.8635 mL 17.7270 mL
5 mM 0.3545 mL 1.7727 mL 3.5454 mL
10 mM 0.1773 mL 0.8864 mL 1.7727 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.43 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Bergman AM, et, al. Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models. Invest New Drugs. 2011 Jun;29(3):456-66.

    [2]. Adema AD, et, al. Cell cycle effects of fatty acid derivatives of cytarabine, CP-4055, and of gemcitabine, CP-4126, as basis for the interaction with oxaliplatin and docetaxel. Int J Oncol. 2010 Jan;36(1):285-94.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Gemcitabine elaidate(Synonyms: 反油酸吉西他滨; CP-4126; CO-101; Gemcitabine 5′-elaidate)

发表于由

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。

Gemcitabine elaidate (Synonyms: 反油酸吉西他滨; CP-4126; CO-101; Gemcitabine 5′-elaidate) 纯度: 98.22%

Gemcitabine elaidate (CP-4126) 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate 具有抗肿瘤活性。

Gemcitabine elaidate(Synonyms: 反油酸吉西他滨; CP-4126; CO-101; Gemcitabine 5

Gemcitabine elaidate Chemical Structure

CAS No. : 210829-30-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1219 In-stock
5 mg ￥1050 In-stock
10 mg ￥1450 In-stock
50 mg ￥4450 In-stock
100 mg ￥6680 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Gemcitabine elaidate 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

Gemcitabine elaidate (CP-4126) is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity[1][2].

体外研究
(In Vitro)

Gemcitabine elaidate (0.2 nM-1 mM; 72 h) inhibits the growth of gemcitabine sensitive and resistant cells, with IC50s of 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4 and MOLT4/C8 cells, respectively[1].
Gemcitabine elaidate (0.5 nM-1 μM; 72 h) increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells[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 Viability Assay[2]

Cell Line: A549 and WiDR cells[2]
Concentration: 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM
Incubation Time: 72 h
Result: Induced a G2/M and S phase accumulation.

体内研究
(In Vivo)

Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) inhibits the solid tumor xenografts growth of non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), pancreatic cancer (PANC-1)[1].
Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) shows acceptable toxicity and significant antitumor activity in the colon cancer xenograft Co6044 bearing mice[1].
Gemcitabine elaidate (p.o. once daily for 5 doses) shows a favorable toxicity and antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044[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.

Animal Model: Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively[1]
Dosage: 25-120 mg/kg
Administration: I.p. every 3 days for 5 doses
Result: Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.

Clinical Trial

分子量

527.64

Formula

C27H43F2N3O5
CAS 号

210829-30-4
中文名称

反油酸吉西他滨
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 : ≥ 26 mg/mL (49.28 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8952 mL 9.4762 mL 18.9523 mL
5 mM 0.3790 mL 1.8952 mL 3.7905 mL
10 mM 0.1895 mL 0.9476 mL 1.8952 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 (4.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.74 mM，饱和度未知) 的澄清溶液。

    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 (4.74 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.74 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 (4.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.74 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]. Bergman AM, et, al. Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models. Invest New Drugs. 2011 Jun;29(3):456-66.

    [2]. Adema AD, et, al. Cell cycle effects of fatty acid derivatives of cytarabine, CP-4055, and of gemcitabine, CP-4126, as basis for the interaction with oxaliplatin and docetaxel. Int J Oncol. 2010 Jan;36(1):285-94.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务