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