标签归档：hjc

HJC0197

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。

HJC0197  纯度: 98.64%

HJC0197 是一种有效的 Epac1 (cAMP 1 直接激活的交换蛋白) 和 Epac2 (对 Epac2 的 IC50=5.9 μM) 拮抗剂。HJC0197 选择性阻断 cAMP 诱导的 Epac 活化。HJC0197 在等浓度 cAMP 存在下抑制 Epac1 介导的 Rap1-GDP 交换活性。

HJC0197

HJC0197 Chemical Structure

CAS No. : 1383539-73-8

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 ￥1100 In-stock
5 mg ￥1000 In-stock
10 mg ￥1600 In-stock
50 mg ￥4500 In-stock
100 mg ￥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

HJC0197 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Anti-Cardiovascular Disease Compound Library
  • Ferroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[1].

体外研究
(In Vitro)

HJC0197 (25 μM) also inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[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

339.45

Formula

C19H21N3OS
CAS 号

1383539-73-8
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 : 50 mg/mL (147.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9459 mL 14.7297 mL 29.4594 mL
5 mM 0.5892 mL 2.9459 mL 5.8919 mL
10 mM 0.2946 mL 1.4730 mL 2.9459 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 (7.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.36 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 (7.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.36 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 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 (7.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.36 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]. Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43.

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HJC0152 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。

HJC0152 hydrochloride  纯度: 98.95%

HJC0152 hydrochloride 是信号转导和转录激活因子 3 (STAT3) 的抑制剂。

HJC0152 hydrochloride

HJC0152 hydrochloride Chemical Structure

CAS No. : 1420290-99-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥700 In-stock
10 mg ￥1100 In-stock
25 mg ￥2100 In-stock
50 mg ￥3500 In-stock
100 mg ￥6200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

HJC0152 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library

生物活性

HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.

IC50 & Target

STAT3

 

体外研究
(In Vitro)

HJC0152 hydrochloride (compound 11) significantly inhibits cell proliferation and induces apoptosis accompanying cellular morphological changes at concentrations of 1, 5, and 10 μM. Results show that treatment with 10 μM HJC0152 hydrochloride decreases the STAT3 promoter activity in MDA-MB-231 cells by approximately 32%, and increasing the dose of HJC0152 hydrochloride to 20 μM further decreases STAT3 promoter activity by 62% as compare with control. Total STAT3 is reduced after treatment with HJC0152 hydrochloride. HJC0152 hydrochloride induces cleaved caspase-3 and down regulates cyclin D1 in MDA-MB-231 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.
体内研究
(In Vivo)

Mice treated with 7.5 mg/kg of HJC0152 hydrochloride (compound 11) via ip show a better effect in inhibiting tumor growth. The growth of xenograft tumors in mice is significantly reduced by HJC0152 hydrochloride at a dose of 25 mg/kg. It is also noteworthy that HJC0152 hydrochloride does not show significant signs of toxicity at a dose of 75 mg/kg[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

406.65

Formula

C15H14Cl3N3O4
CAS 号

1420290-99-8
运输条件

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

4°C, sealed storage, away from moisture

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

DMSO : 1 mg/mL (2.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4591 mL 12.2956 mL 24.5912 mL
5 mM — — —
10 mM — — —

*

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)。-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。
参考文献

  • [1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
Cell Assay
[1]

Breast cancer MDA-MB-231 cells are incubated in 6-well plates (2.5×105/well). Cells are then treated with DMSO, or HJC0152 hydrochloride (compound 11) at different concentrations for 48 h, and then both adherent and floating cells are collected, washed once with PBS. Resuspended cells are incubated with 100 μL PBS containing 1% BSA and 100 μL Annexin V and dead cell detection reagent at room temperature for 20 min. Apoptosis is measured immediately using the Muse Cell Analyzer with the MuseTM Apoptosis Kit[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 Administration
[1]

Fifty-four female nude mice are are used for orthotopic tumor studies at 4 to 6 weeks of age. The mice are maintained in a barrier unit with 12 h light-dark switch. Freshly harvested MDA-MB-231 cells (2.5×106 cells per mouse, resuspended in 100 μL PBS) are injected into the 3rd mammary fat pad of the mice, and then randomly assigned into 8 groups (5 to10 mice per group). For the intraperitoneal treatment experiment, the mice are treated daily with 2.5 mg/kg HJC0152 hydrochloride (compound 11) (Group A) or vehicle (Group D) when the tumor volume reaches 200 mm3. A Body weights and tumors volume are measured daily and tumor volume is calculated according to the formula V=0.5×L×W2, where L=length (mm) and W=width (mm)[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.
参考文献

  • [1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.

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

HJC0350

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。

HJC0350  纯度: 99.52%

HJC0350是有效选择性的EPAC2拮抗剂，IC50值为0.3 µM。

HJC0350

HJC0350 Chemical Structure

CAS No. : 885434-70-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥800 In-stock
25 mg ￥1700 In-stock
50 mg ￥2800 In-stock
100 mg ￥4800 In-stock
200 mg ￥7700 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

HJC0350 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.

IC50 & Target

IC50: 0.3 µM (EPAC2)[1]
体外研究
(In Vitro)

HJC0350 has an apparent IC50 value of 0.3 µM for competing with 8-NBD-cAMP binding of EPAC2, and is about 133-fold more potent than cAMP. HJC0350 is found not to inhibit EPAC1-mediated Rap1-GDP exchange activity at 25 µM in the presence of equal concentration of cAMP, indicating that it is EPAC2-specific antagonists. Pretreatment of HEK293/EPAC2-FL cells with 10 µM HJC0350 fully blocks the 007-AM induced decrease of FRET[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

277.38

Formula

C15H19NO2S
CAS 号

885434-70-8
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 : 33.33 mg/mL (120.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6052 mL 18.0258 mL 36.0516 mL
5 mM 0.7210 mL 3.6052 mL 7.2103 mL
10 mM 0.3605 mL 1.8026 mL 3.6052 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 (9.01 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.01 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]. Chen H, et al. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem. 2013 Feb 14;56(3):952-62.

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

HJC0416 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。

HJC0416 hydrochloride 

HJC0416 hydrochloride 是一种有效的口服活性 STAT3 抑制剂，具有比 Stattic (HY-13818) 更强的抗癌活性。HJC0416 hydrochloride 是一种很有前途的抗乳腺癌试剂。

HJC0416 hydrochloride

HJC0416 hydrochloride Chemical Structure

CAS No. : 2415263-08-8

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

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].
HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].
HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].
HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[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: MDA-MB-231 breast cancer cells
Concentration: 1-10 µM
Incubation Time: 48 hours
Result: Induced cell apoptosis in cancer cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 12 hours
Result: Decreased p-STAT3 phosphorylation expression and cyclin D1 level.

体内研究
(In Vivo)

HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].

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

Animal Model: Mice with MDA-MB-231 cells[1]
Dosage: 10 mg/kg (i.p.); 100 mg/kg (oral)
Administration: Intraperitoneal injection, 7 days; oral administration, 14 days
Result: Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.

分子量

429.32

Formula

C18H18Cl2N2O4S
CAS 号

2415263-08-8
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.
溶解性数据
In Vivo:
  • 1.

    All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献

  • [1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.

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

HJC0416 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。

HJC0416 hydrochloride 

HJC0416 hydrochloride 是一种有效的口服活性 STAT3 抑制剂，具有比 Stattic (HY-13818) 更强的抗癌活性。HJC0416 hydrochloride 是一种很有前途的抗乳腺癌试剂。

HJC0416 hydrochloride

HJC0416 hydrochloride Chemical Structure

CAS No. : 2415263-08-8

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

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].
HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].
HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].
HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 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.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1-10 µM
Incubation Time: 48 hours
Result: Induced cell apoptosis in cancer cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 12 hours
Result: Decreased p-STAT3 phosphorylation expression and cyclin D1 level.

体内研究
(In Vivo)

HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[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: Mice with MDA-MB-231 cells[1]
Dosage: 10 mg/kg (i.p.); 100 mg/kg (oral)
Administration: Intraperitoneal injection, 7 days; oral administration, 14 days
Result: Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.

分子量

429.32

Formula

C18H18Cl2N2O4S
CAS 号

2415263-08-8
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.
溶解性数据
In Vivo:
  • 1.

    All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献

  • [1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.

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HJC0416 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。

HJC0416 hydrochloride 

HJC0416 hydrochloride 是一种有效的口服活性 STAT3 抑制剂，具有比 Stattic (HY-13818) 更强的抗癌活性。HJC0416 hydrochloride 是一种很有前途的抗乳腺癌试剂。

HJC0416 hydrochloride

HJC0416 hydrochloride Chemical Structure

CAS No. : 2415263-08-8

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生物活性

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].
HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].
HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].
HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[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: MDA-MB-231 breast cancer cells
Concentration: 1-10 µM
Incubation Time: 48 hours
Result: Induced cell apoptosis in cancer cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 12 hours
Result: Decreased p-STAT3 phosphorylation expression and cyclin D1 level.

体内研究
(In Vivo)

HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].

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

Animal Model: Mice with MDA-MB-231 cells[1]
Dosage: 10 mg/kg (i.p.); 100 mg/kg (oral)
Administration: Intraperitoneal injection, 7 days; oral administration, 14 days
Result: Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.

分子量

429.32

Formula

C18H18Cl2N2O4S
CAS 号

2415263-08-8
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.
溶解性数据
In Vivo:
  • 1.

    All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献

  • [1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.

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