标签归档：minnelide

Minnelide-d3

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。

Minnelide-d3 

Minnelide-d3 是 Minnelide 的氘代物。Minnelide 是雷公藤内酯的衍生物，在许多肿瘤类型 (特别是在胰腺癌) 中显示出抗肿瘤 (antitumor) 活性。 Minnelide 可导致凋亡 (apoptosis)。

Minnelide-d3

Minnelide-d3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Minnelide-d3 is the deuterium labeled Minnelide. Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

517.39

Formula

C21H22D3Na2O10P
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Noel P, et al. Triptolide and Its Derivatives as Cancer Therapies. Trends Pharmacol Sci. 2019 May;40(5):327-341.

    [3]. Chugh R, et al. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci Transl Med. 2012 Oct 17;4(156):156ra139.

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

Minnelide-d3

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。

Minnelide-d3 

Minnelide-d3 是 Minnelide 的氘代物。Minnelide 是雷公藤内酯的衍生物，在许多肿瘤类型 (特别是在胰腺癌) 中显示出抗肿瘤 (antitumor) 活性。 Minnelide 可导致凋亡 (apoptosis)。

Minnelide-d3

Minnelide-d3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Minnelide-d3 is the deuterium labeled Minnelide. Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

517.39

Formula

C21H22D3Na2O10P
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Noel P, et al. Triptolide and Its Derivatives as Cancer Therapies. Trends Pharmacol Sci. 2019 May;40(5):327-341.

    [3]. Chugh R, et al. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci Transl Med. 2012 Oct 17;4(156):156ra139.

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

Minnelide-d3

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。

Minnelide-d3 

Minnelide-d3 是 Minnelide 的氘代物。Minnelide 是雷公藤内酯的衍生物，在许多肿瘤类型 (特别是在胰腺癌) 中显示出抗肿瘤 (antitumor) 活性。 Minnelide 可导致凋亡 (apoptosis)。

Minnelide-d3

Minnelide-d3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Minnelide-d3 is the deuterium labeled Minnelide. Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[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

517.39

Formula

C21H22D3Na2O10P
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Noel P, et al. Triptolide and Its Derivatives as Cancer Therapies. Trends Pharmacol Sci. 2019 May;40(5):327-341.

    [3]. Chugh R, et al. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci Transl Med. 2012 Oct 17;4(156):156ra139.

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

Minnelide

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。

Minnelide  纯度: 99.59%

Minnelide 是雷公藤内酯的衍生物，在许多肿瘤类型 (特别是在胰腺癌) 中显示出抗肿瘤 (antitumor) 活性。 Minnelide 可导致凋亡 (apoptosis)。

Minnelide

Minnelide Chemical Structure

CAS No. : 1254702-87-8

规格 价格 是否有货 数量
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥8500 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Minnelide 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Anti-Pancreatic Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis[1].

体外研究
(In Vitro)

Minnelide (0-200 nM; 48 hours) shows significantly decreased cell viability in pancreatic cancer cell lines after treatment in the presence, but not in the absence, of phosphatase[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: Pancreatic cancer cell line: S2-013, MIA PaCa-2, S2-VP10, and Panc-1 cells
Concentration: 0.100 nM, 200 nM
Incubation Time: 48 hours
Result: Decreased cell viability of in vitro.

体内研究
(In Vivo)

Minnelide (injection intraperitoneally; 0.1-0.6 mg/kg; once daily or twice daily) leads to a marked decrease in tumor weight and volume at the end of treatment and increases survival in orthotopic model of pancreatic cancer with MIA PaCa-2–derived human pancreatic tumors[2].
Minnelide (injection intraperitoneally; 0.42 mg/kg; once daily; 28 days) prevents locoregional spread and leads to a decrease in average tumor weight in a xenograft model of pancreatic cancer with metastatic S2-013 cells[2].
Minnelide (injection intraperitoneally; 0.42 mg/kg, 0.21 mg/kg; once daily) causes tumor regression and tumors from Minnelide-treated animals showed fibrosis and the presence of pyknotic nuclei in human pancreatic cancer xenografts in SCID mice[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.

Animal Model: Orthotopic model of pancreatic cancer with MIA PaCa 2-derived human pancreatic tumors in athymic nude mice[2]
Dosage: 0.1-0.6 mg/kg
Administration: Injection intraperitoneally; 0.1-0.6 mg/kg; once daily or twice daily
Result: Prevented pancreatic tumor growth in vivo.
Animal Model: Xenograft model of pancreatic cancer with metastatic S2-013 cell line in athymic nude mice[2]
Dosage: 0.42 mg/kg
Administration: Injection intraperitoneally; 0.42 mg/kg; once daily
Result: Prevented extensive spread from the primary site of injection.
Animal Model: Human pancreatic cancer xenografts in SCID mice[2]
Dosage: 0.21 mg/kg, 0.42 mg/kg
Administration: Injection intraperitoneally; 0.42 mg/kg; once daily
Result: Reduced tumor burden in human xenografts from patients.

Clinical Trial

分子量

514.37

Formula

C21H25Na2O10P
CAS 号

1254702-87-8
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 : 16.67 mg/mL (32.41 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9441 mL 9.7206 mL 19.4413 mL
5 mM 0.3888 mL 1.9441 mL 3.8883 mL
10 mM 0.1944 mL 0.9721 mL 1.9441 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.25 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 16.7 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]. Noel P, et al. Triptolide and Its Derivatives as Cancer Therapies. Trends Pharmacol Sci. 2019 May;40(5):327-341.

    [2]. Chugh R, et al. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci Transl Med. 2012 Oct 17;4(156):156ra139.

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