标签归档：抑制

Linderalactone

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。

Linderalactone  纯度: ≥98.0%

Linderalactone 是从 Radix linderae 中分离出来的一种重要的倍半萜烯内酯。Linderalactone 通过调节凋亡相关蛋白的表达和抑制 JAK/STAT 信号通路来抑制癌细胞生长。Linderalactone 还以 IC50 值为 15 µM 来抑制肺癌 A-549 细胞的增殖。

Linderalactone

Linderalactone Chemical Structure

CAS No. : 728-61-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1800 In-stock
5 mg ￥2020 In-stock
10 mg ￥3430 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Linderalactone 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Macrocyclic Compound Library
  • Terpenoids Library
  • Traditional Chinese Medicine Monomer Library
  • Anti-Lung Cancer Compound Library

生物活性

Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM[1][2].

体外研究
(In Vitro)

Linderalactone (0-100 μM; 24 hours; A549 cells) treatment inhibits the growth of A549 cells concentration-dependently. The IC50 of linderalactone is 15 µM[1].
Linderalactone (7.5-30 μM; A549 cells) treatment induces apoptosis in A549 cells in a dose-dependent manner[1].
Linderalactone (7.5-30 μM; 24 hours; A549 cells) treatment induces G2/M cell cycle arrest of A549 cells dose-dependently[1].
Linderalactone (7.5-30 μM; A549 cells) inhibits the expression of STAT1, JAK1 and JAK2. Linderalactone could also inhibit the phosphorylation of pSTAT1, pSTAT-2, pJAK1 and pJAk2[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[1]

Cell Line: Lung cancer A549 cells
Concentration: 0 μM, 1.6 μM, 3.2 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 24 hours
Result: Inhibited the growth of A549 cells concentration-dependently.

Apoptosis Analysis[1]

Cell Line: Lung cancer A549 cells
Concentration: 7.5 μM, 15 μM, 30 μM
Incubation Time:
Result: Induced apoptosis in A549 cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: Lung cancer A549 cells
Concentration: 7.5 μM, 15 μM, 30 μM
Incubation Time: 24 hours
Result: Induced G2/M cell cycle arrest.

Western Blot Analysis[1]

Cell Line: Lung cancer A549 cells
Concentration: 7.5 μM, 15 μM, 30 μM
Incubation Time:
Result: Inhibited the JAK/STAT pathway in A549 cells.

分子量

244.29

Formula

C15H16O3
CAS 号

728-61-0
运输条件

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

-20°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 : 33.33 mg/mL (136.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0935 mL 20.4675 mL 40.9350 mL
5 mM 0.8187 mL 4.0935 mL 8.1870 mL
10 mM 0.4093 mL 2.0467 mL 4.0935 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： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (10.23 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (10.23 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 (10.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.23 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]. Deng Y, et al. Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins, G2/M cell cycle arrest and inhibition of JAK/STAT signalling pathway. J BUON. 2019 Mar-Apr;24(2):566-571.

    [2]. Qinghua Sun, et al. Preparative Isolation and Purification of Linderalactone and Lindenenol from Radix linderae by HSCCC. Journal of Liquid Chromatography & Related Technologies. Aug 2005:113-121.

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

Cynaropicrin

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。

Cynaropicrin  纯度: 97.16%

Cynaropicrin 是一种倍半萜内酯，可以抑制肿瘤坏死因子 (TNF-α) 的释放，在鼠和人巨噬细胞的 IC50 值分别为 8.24 和 3.18 μM。 Cynaropicrin 也抑制软骨降解因子 (MMP13) 的增加并抑制 NF-κB 的信号传导。

Cynaropicrin

Cynaropicrin Chemical Structure

CAS No. : 35730-78-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4950 In-stock
5 mg ￥4500 In-stock
10 mg ￥6500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Cynaropicrin 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Terpenoids Library
  • Pyroptosis Compound Library
  • Traditional Chinese Medicine Monomer Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Food-Sourced Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.

IC50 & Target[1][2]

MMP13

 

NF-κB

 

TNF-α

 

体外研究
(In Vitro)

Cynaropicrin strongly inhibits lipopolysaccharide-induced TNF-α release from either murine or human macrophage cells in a dose-dependent manner with the IC50 values of 8.24 and 3.18 μM, respectively. Cynaropicrin shows significant inhibitory effects toward all mitogenic signals with the IC50 values of 1.20 (concanavalin A), 1.02 (phytohemagglutinin) and 0.90 μM (lipopolysaccharide), respectively. Cynaropicrin suppresses CTLL-2 cell proliferation in a dose-dependent manner and the 50% inhibitory concentration (IC50) of Cynaropicrin for CTLL-2 cell growth is 0.91 μM[1]. The increased mRNA expression of MMP13 induced by TNF-α is similarly inhibited in a concentration-dependent manner by Cynaropicrin. The increased mRNA expression of HIF-2α induced by IL-1β in SW1353 is inhibited in a concentration-dependent manner by Cynaropicrin[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.
分子量

346.37

Formula

C19H22O6
CAS 号

35730-78-0
运输条件

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

-20°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 : ≥ 50 mg/mL (144.35 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 2.8871 mL 14.4354 mL 28.8709 mL
5 mM 0.5774 mL 2.8871 mL 5.7742 mL
10 mM 0.2887 mL 1.4435 mL 2.8871 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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.22 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 (7.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.22 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 (7.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.22 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]. Cho JY, et al. In vitro anti-inflammatory effects of cynaropicrin, a sesquiterpene lactone, from Saussurea lappa. Eur J Pharmacol. 2000 Jun 23;398(3):399-407.

    [2]. Masutani T, et al. Cynaropicrin is dual regulator for both degradation factors and synthesis factors in the cartilage metabolism. Life Sci. 2016 Aug 1;158:70-7.

    [3]. da Silva CF, et al. Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo. Antimicrob Agents Chemother. 2013 Nov;57(11):5307-14.
Cell Assay
[1]

Human U937 cells are cultured in RPMI1640 supplemented with 10% fetal bovine serum. To differentiate U937 cells, 2×106 cells/mL are treated with phorbol 12-myristate 13-acetate (PMA) of 20 ng/mL for 24 h. The PMA is removed by washing and adherent cells are then allowed to recuperate for 40 h. The recuperated cells are subsequently incubated with lipopolysaccharide of 1 μg/mL for 6 h with Cynaropicrin and positive control drugs. Supernatants are harvested and assayed by ELISA kit for human TNF-α[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
[3]

Male Swiss mice are used in this study. Mice are housed at a maximum of 8 per cage and kept in a conventional room at 20 to 24°C under a 12 h to 12 h light-dark cycle. The animals are provided with sterilized water and chow ad libitum. Infection is performed by i.p. injection of 104 or 5×103 bloodstream trypomastigotes. The animals (18 to 21 g) are divided into the following groups (at least five mice per group): uninfected (noninfected and untreated), untreated (infected with T. cruzi but treated only with vehicle), and treated (infected and treated i.p. with 0.5 to 50 mg/kg/day compound (including Cynaropicrin) or 100 mg/kg/day benznidazole). Mice receive 0.1 mL (i.p.) at 5 and 8 days postinfection (dpi), or at 11, 12, and 13 dpi for the dose of 25 mg/kg, twice a day (b.i.d.)[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.
参考文献

  • [1]. Cho JY, et al. In vitro anti-inflammatory effects of cynaropicrin, a sesquiterpene lactone, from Saussurea lappa. Eur J Pharmacol. 2000 Jun 23;398(3):399-407.

    [2]. Masutani T, et al. Cynaropicrin is dual regulator for both degradation factors and synthesis factors in the cartilage metabolism. Life Sci. 2016 Aug 1;158:70-7.

    [3]. da Silva CF, et al. Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo. Antimicrob Agents Chemother. 2013 Nov;57(11):5307-14.

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

Aminopurvalanol A

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。

Aminopurvalanol A  纯度: 98.00%

Aminopurvalanol A 是一种有效的、选择性的、可渗透细胞的 Cyclins/Cdk 复合物抑制剂。Aminopurvalanol A 优先靶向G2/M 期转变进而抑制癌细胞分化。Aminopurvalanol A 通过抑制生理获能依赖性肌动蛋白聚合而抑制精子受精能力。

Aminopurvalanol A

Aminopurvalanol A Chemical Structure

CAS No. : 220792-57-4

规格 价格 是否有货 数量
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
25 mg ￥3900 In-stock
50 mg ￥6000 In-stock
100 mg ￥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Aminopurvalanol A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization[1][2].

IC50 & Target

Cyclins/Cdk[1]
体外研究
(In Vitro)

Aminopurvalanol A (5 and 40 μM; 8 hours) inhibits cell growth primarily by arresting the cells in the G2 phase of the cell cycle and, at higher concentration, triggering apoptosis[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: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: Increased the number of cells with a 4N DNA content as early as 8 h after the beginning of treatment at 5 μM. 40 μM led to cellular fragmentation and cells with an irregular DNA distribution, characteristic of apoptotic cell populations.

Apoptosis Analysis[2]

Cell Line: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: 40 μM Aminopurvalanol A led to apoptosis rather than after the beginning of treatment at 5 μM.

分子量

403.91

Formula

C19H26ClN7O
CAS 号

220792-57-4
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 (247.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4758 mL 12.3790 mL 24.7580 mL
5 mM 0.4952 mL 2.4758 mL 4.9516 mL
10 mM 0.2476 mL 1.2379 mL 2.4758 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 (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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]. Bernabò N, et al. Aminopurvalanol A, a Potent, Selective, and Cell Permeable Inhibitor of Cyclins/Cdk Complexes, Causes the Reduction of in Vitro Fertilizing Ability of Boar Spermatozoa, by Negatively Affecting the Capacitation-Dependent Actin Polymerization. Front Physiol. 2017;8:1097.

    [2]. Rosania GR, et al. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999;96(9):4797-4802.

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

Aminopurvalanol A

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。

Aminopurvalanol A  纯度: 98.00%

Aminopurvalanol A 是一种有效的、选择性的、可渗透细胞的 Cyclins/Cdk 复合物抑制剂。Aminopurvalanol A 优先靶向G2/M 期转变进而抑制癌细胞分化。Aminopurvalanol A 通过抑制生理获能依赖性肌动蛋白聚合而抑制精子受精能力。

Aminopurvalanol A

Aminopurvalanol A Chemical Structure

CAS No. : 220792-57-4

规格 价格 是否有货 数量
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
25 mg ￥3900 In-stock
50 mg ￥6000 In-stock
100 mg ￥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Aminopurvalanol A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization[1][2].

IC50 & Target

Cyclins/Cdk[1]
体外研究
(In Vitro)

Aminopurvalanol A (5 and 40 μM; 8 hours) inhibits cell growth primarily by arresting the cells in the G2 phase of the cell cycle and, at higher concentration, triggering apoptosis[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: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: Increased the number of cells with a 4N DNA content as early as 8 h after the beginning of treatment at 5 μM. 40 μM led to cellular fragmentation and cells with an irregular DNA distribution, characteristic of apoptotic cell populations.

Apoptosis Analysis[2]

Cell Line: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: 40 μM Aminopurvalanol A led to apoptosis rather than after the beginning of treatment at 5 μM.

分子量

403.91

Formula

C19H26ClN7O
CAS 号

220792-57-4
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 (247.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4758 mL 12.3790 mL 24.7580 mL
5 mM 0.4952 mL 2.4758 mL 4.9516 mL
10 mM 0.2476 mL 1.2379 mL 2.4758 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 (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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]. Bernabò N, et al. Aminopurvalanol A, a Potent, Selective, and Cell Permeable Inhibitor of Cyclins/Cdk Complexes, Causes the Reduction of in Vitro Fertilizing Ability of Boar Spermatozoa, by Negatively Affecting the Capacitation-Dependent Actin Polymerization. Front Physiol. 2017;8:1097.

    [2]. Rosania GR, et al. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999;96(9):4797-4802.

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

Aminopurvalanol A

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。

Aminopurvalanol A  纯度: 98.00%

Aminopurvalanol A 是一种有效的、选择性的、可渗透细胞的 Cyclins/Cdk 复合物抑制剂。Aminopurvalanol A 优先靶向G2/M 期转变进而抑制癌细胞分化。Aminopurvalanol A 通过抑制生理获能依赖性肌动蛋白聚合而抑制精子受精能力。

Aminopurvalanol A

Aminopurvalanol A Chemical Structure

CAS No. : 220792-57-4

规格 价格 是否有货 数量
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
25 mg ￥3900 In-stock
50 mg ￥6000 In-stock
100 mg ￥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Aminopurvalanol A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization[1][2].

IC50 & Target

Cyclins/Cdk[1]
体外研究
(In Vitro)

Aminopurvalanol A (5 and 40 μM; 8 hours) inhibits cell growth primarily by arresting the cells in the G2 phase of the cell cycle and, at higher concentration, triggering apoptosis[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 Cycle Analysis[2]

Cell Line: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: Increased the number of cells with a 4N DNA content as early as 8 h after the beginning of treatment at 5 μM. 40 μM led to cellular fragmentation and cells with an irregular DNA distribution, characteristic of apoptotic cell populations.

Apoptosis Analysis[2]

Cell Line: Human U937 leukemic cells
Concentration: 5 and 40 μM
Incubation Time: 8 hours
Result: 40 μM Aminopurvalanol A led to apoptosis rather than after the beginning of treatment at 5 μM.

分子量

403.91

Formula

C19H26ClN7O
CAS 号

220792-57-4
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 (247.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4758 mL 12.3790 mL 24.7580 mL
5 mM 0.4952 mL 2.4758 mL 4.9516 mL
10 mM 0.2476 mL 1.2379 mL 2.4758 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 (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.19 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]. Bernabò N, et al. Aminopurvalanol A, a Potent, Selective, and Cell Permeable Inhibitor of Cyclins/Cdk Complexes, Causes the Reduction of in Vitro Fertilizing Ability of Boar Spermatozoa, by Negatively Affecting the Capacitation-Dependent Actin Polymerization. Front Physiol. 2017;8:1097.

    [2]. Rosania GR, et al. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999;96(9):4797-4802.

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

YH-306

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。

YH-306 

YH-306 是一种抗肿瘤剂。YH-306 通过 FAK 通路抑制结直肠肿瘤的生长和转移。 YH-306 显着抑制结直肠癌细胞的迁移和侵袭。YH-306 有效抑制不受抑制的增殖并诱导细胞凋亡 (apoptosis)。YH-306 抑制 FAK、c-Src、桩蛋白和 PI3K、Rac1 的激活以及 MMP2 和 MMP9 的表达。YH-306 还抑制肌动蛋白相关蛋白 (Arp2/3) 复合物介导的肌动蛋白聚合。

YH-306

YH-306 Chemical Structure

CAS No. : 1373764-75-0

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

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization[1].

IC50 & Target[1]

PI3K

 

MMP2

 

MMP9

 

分子量

306.36

Formula

C19H18N2O2
CAS 号

1373764-75-0
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]. Dai F, et al. A novel synthetic small molecule YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. J Cell Mol Med. 2015 Feb;19(2):383-95.

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

YH-306

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。

YH-306 

YH-306 是一种抗肿瘤剂。YH-306 通过 FAK 通路抑制结直肠肿瘤的生长和转移。 YH-306 显着抑制结直肠癌细胞的迁移和侵袭。YH-306 有效抑制不受抑制的增殖并诱导细胞凋亡 (apoptosis)。YH-306 抑制 FAK、c-Src、桩蛋白和 PI3K、Rac1 的激活以及 MMP2 和 MMP9 的表达。YH-306 还抑制肌动蛋白相关蛋白 (Arp2/3) 复合物介导的肌动蛋白聚合。

YH-306

YH-306 Chemical Structure

CAS No. : 1373764-75-0

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

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization[1].

IC50 & Target[1]

PI3K

 

MMP2

 

MMP9

 

分子量

306.36

Formula

C19H18N2O2
CAS 号

1373764-75-0
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]. Dai F, et al. A novel synthetic small molecule YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. J Cell Mol Med. 2015 Feb;19(2):383-95.

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

YH-306

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。

YH-306 

YH-306 是一种抗肿瘤剂。YH-306 通过 FAK 通路抑制结直肠肿瘤的生长和转移。 YH-306 显着抑制结直肠癌细胞的迁移和侵袭。YH-306 有效抑制不受抑制的增殖并诱导细胞凋亡 (apoptosis)。YH-306 抑制 FAK、c-Src、桩蛋白和 PI3K、Rac1 的激活以及 MMP2 和 MMP9 的表达。YH-306 还抑制肌动蛋白相关蛋白 (Arp2/3) 复合物介导的肌动蛋白聚合。

YH-306

YH-306 Chemical Structure

CAS No. : 1373764-75-0

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

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization[1].

IC50 & Target[1]

PI3K

 

MMP2

 

MMP9

 

分子量

306.36

Formula

C19H18N2O2
CAS 号

1373764-75-0
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]. Dai F, et al. A novel synthetic small molecule YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. J Cell Mol Med. 2015 Feb;19(2):383-95.

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

Imatinib(Synonyms: 伊马替尼; STI571; CGP-57148B)

发表于由

Imatinib (Synonyms: 伊马替尼; STI571; CGP-57148B) 纯度: 99.54%

Imatinib (STI571) 是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL，v-Abl，PDGFR，c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合，将其锁定在封闭或自我抑制的构象中，因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和 MERS-CoV。

Imatinib(Synonyms: 伊马替尼; STI571; CGP-57148B)

Imatinib Chemical Structure

CAS No. : 152459-95-5

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 ￥550 In-stock
200 mg ￥500 In-stock
500 mg ￥900 In-stock
1 g ￥1520 In-stock
5 g ￥4950 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

Imatinib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Reprogramming Compound Library
  • NMPA-Approved Drug Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Alzheimer’s Disease Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Therapy Drug Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively[1][2][3][4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV[5].

IC50 & Target

BCR/ABL, v-Abl, PDGFR, c-kit[1][2][4]
体外研究
(In Vitro)

Imatinib (STI571) inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM[1].
Imatinib (STI571) is very effective (in vitro IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) and PDGFR (in vitro IC50, 380 nM)[2].
Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[4].
The IC50s of Imatinib(STI571) is a multi-target inhibitor of v-Abl, c-Kit and on BON-1 and H727 cells after exposure for 48 h are 32.4 and 32.8 μM, respectively[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In the phosphorothioate antisense oligodeoxynucleotides (PS-ASODN) group, tumor growth is inhibited by 59.437%, which is markedly higher than in the Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and group (11.071%) and liposome negative control group (2.759%). Telomerase activity is significantly lower (P<0.01) in the PS-ASODN group (0.689±0.158) compare with the Imatinib group (1.838±0.241), liposome negative control group (2.013±0.273), and saline group (2.004±0.163)[7].
Imatinib (25 mg/kg/day, p.o.) suppresses the growth of endometriotic tissue and reduces the number of ovarian follicles in a rat model. Imatinib effectively treats experimental endometriosis by its inhibitor effects on angiogenesis and cell proliferation[8].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

493.60

Formula

C29H31N7O
CAS 号

152459-95-5
中文名称

伊马替尼
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 : 12.5 mg/mL (25.32 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0259 mL 10.1297 mL 20.2593 mL
5 mM 0.4052 mL 2.0259 mL 4.0519 mL
10 mM 0.2026 mL 1.0130 mL 2.0259 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： 0.5% CMC-Na/saline water

    Solubility: 11 mg/mL (22.29 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.53 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.53 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.53 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 12.5 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 MCE 网站选购。
参考文献

  • [1]. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.

    [2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.

    [3]. Iqbal N, et al. Imatinib: a breakthrough of targeted therapy in cancer. Chemother Res Pract. 2014;2014:357027.

    [4]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8

    [5]. Jeanne M Sisk, et al. Coronavirus S Protein-Induced Fusion Is Blocked Prior to Hemifusion by Abl Kinase Inhibitors. J Gen Virol. 2018 May;99(5):619-630.

    [6]. Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13(1):234-40.

    [7]. Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013 Apr 21;19(15):2340-7.

    [8]. Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.

    [9]. Coleman CM, et al, Frieman MB. Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion. J Virol. 2016;90(19):8924‐8933. Published 2016 Sep 12.
Cell Assay
[4]

BON-1 cells (7,500 per well) and NCI-H727 cells (5,000 per well) are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 h (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated. Experiments are done in triplicates[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[6][7]

Mice[6]
The 40 tumor-bearing SCID mice are randomly divided into four groups (10 mice per group): the PS-ASODN group (5 μM, each mouse receives 0.2 mL by intratumor injection once daily); Imatinib group (0.1 mg/g body weight); liposome negative control group (0.01 mL/g); and saline group (0.01 mL/g). The mice in each group receive the relevant treatment by intra-tumor injection once daily from day 7 to day 28 after implantation. After 28 d, the mice are sacrificed, and tumor weight and longest and shortest diameters are measured by electronic scale and vernier caliper, respectively. Inhibition of tumor growth is calculated.
Rats[7]
Adult female Wistar-Albino rats (220-240 g) are used. Twenty-one days after the first surgical procedure, the rats undergo a second laparotomy to evaluate the occurrence of endometriosis. Twenty-four rats have visually confirmed endometriotic implants and are randomized into three groups to receive Imatinib (25 mg/kg/day, p.o.), Anastrozole (0.004 mg/day, p.o.), or normal saline (0.1 mL, i.p.) for 14 days.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.

    [2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.

    [3]. Iqbal N, et al. Imatinib: a breakthrough of targeted therapy in cancer. Chemother Res Pract. 2014;2014:357027.

    [4]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8

    [5]. Jeanne M Sisk, et al. Coronavirus S Protein-Induced Fusion Is Blocked Prior to Hemifusion by Abl Kinase Inhibitors. J Gen Virol. 2018 May;99(5):619-630.

    [6]. Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13(1):234-40.

    [7]. Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013 Apr 21;19(15):2340-7.

    [8]. Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.

    [9]. Coleman CM, et al, Frieman MB. Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion. J Virol. 2016;90(19):8924‐8933. Published 2016 Sep 12.

SCH772984

发表于由

SCH772984  纯度: 98.69%

SCH772984 是一种高选择性和 ATP 竞争性 ERK 抑制剂，对 ERK1 和 ERK2 的 IC50 分别为 4 和 1 nM。SCH772984 在对天然 MAPK 抑制和耐药 MAPK 抑制的细胞中的 BRAF 或 RAS 突变，具有抗肿瘤活性。

SCH772984

SCH772984 Chemical Structure

CAS No. : 942183-80-4

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 ￥2044 In-stock
2 mg ￥1050 In-stock
5 mg ￥1581 In-stock
10 mg ￥2046 In-stock
50 mg ￥7254 In-stock
100 mg ￥10602 In-stock
200 mg ￥14000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

SCH772984 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Chemical Probe Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations[1].

IC50 & Target[1]

ERK2

1 nM (IC50)

ERK1

4 nM (IC50)

体外研究
(In Vitro)

SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells[1].
SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation[1].
SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: LOX cells (SCH772984-sensitive melanoma cells)
Concentration: 300 nM
Incubation Time: 24, 48 hours
Result: Revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis.

Western Blot Analysis[1]

Cell Line: LOX BRAFV600E melanoma cells
Concentration: 3, 10, 30, 100, 300 nM
Incubation Time: 24 hours
Result: A dose-dependent inhibition of phosphorylation of the ERK substrate RSK (T359/S363 phospho-RSK), and also inhibited phosphorylation of residues in the activation loop of ERK itself (T202/Y204 and T185/Y187 of ERK1 and ERK2, respectively).

体内研究
(In Vivo)

SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression[1].
Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice bearing human LOX BRAFV600E tumors[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: Intraperitoneal injection; twice daily for 14 days
Result: Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg).

分子量

587.67

Formula

C33H33N9O2
CAS 号

942183-80-4
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 : 48 mg/mL (81.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7016 mL 8.5082 mL 17.0164 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 mL
10 mM 0.1702 mL 0.8508 mL 1.7016 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： 20% SBE-β-CD adjusted to pH 4-4.5 with 1 N acetic

    Solubility: 20 mg/mL (34.03 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: ≥ 2.4 mg/mL (4.08 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (2.43 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 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

  • 4.

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

    Solubility: 1.43 mg/mL (2.43 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.43 mg/mL (2.43 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 14.3 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
  • 5.

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

    Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (2.43 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 14.3 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 MCE 网站选购。
参考文献

  • [1]. Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50.

PTC299

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。

PTC299  纯度: 99.52%

PTC299 是 VEGFA mRNA 翻译的具有口服活性抑制剂，在转录后水平选择性地抑制 VEGF 蛋白的合成。PTC299 也是二氢乳酸盐脱氢酶 (DHODH) 的有效抑制剂。PTC299 良好的口服生物利用度，缺乏脱靶激酶抑制和骨髓抑制。PTC299 可用于血液系统恶性肿瘤的研究。

PTC299

PTC299 Chemical Structure

CAS No. : 1256565-36-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4180 In-stock
5 mg ￥3800 In-stock
10 mg ￥5700 In-stock
25 mg ￥10500 In-stock
50 mg ￥16400 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PTC299 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Mitochondria-Targeted Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies[1][2].

IC50 & Target

VEGF[2]
体外研究
(In Vitro)

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM[1].
PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia 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.
Clinical Trial

分子量

467.34

Formula

C25H20Cl2N2O3
CAS 号

1256565-36-2
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 (106.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1398 mL 10.6988 mL 21.3977 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 mL
10 mM 0.2140 mL 1.0699 mL 2.1398 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: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.78 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 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% corn oil

    Solubility: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.78 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 8.3 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]. Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18(1):3-16.

    [2]. Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi’s Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7.

    [3]. Packer RJ, et al. Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015;121(1):217-224.

    [4]. Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103(9):1415-1417.

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

(Z)-Guggulsterone

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。

(Z)-Guggulsterone  纯度: 98.43%

Z-guggulsterone 是印度阿育吠陀药用植物 Commiphora mukul 的成分，通过引起细胞凋亡 (apoptosis) 来抑制人前列腺癌细胞的生长。 Z-guggulsterone 通过抑制 VEGF-VEGF-R2-Akt 信号传导轴来抑制血管生成。

(Z)-Guggulsterone

(Z)-Guggulsterone Chemical Structure

CAS No. : 39025-23-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2200 In-stock
5 mg ￥1300 In-stock
10 mg ￥2000 In-stock
25 mg ￥4000 In-stock
50 mg ￥6200 In-stock
100 mg ￥8800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

(Z)-Guggulsterone 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Protein Tyrosine Kinase Compound Library
  • Stem Cell Signaling Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Lipid Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis[1].

IC50 & Target[1]

VEGF-R2

 

Akt

 

体外研究
(In Vitro)

Z-guggulsterone (10, 20 μM; 24 or 48 hours) causes a decrease in the level of VEGF-R2 protein in HUVEC[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.

Western Blot Analysis[1]

Cell Line: Vascular endothelial growth factor (VEGF)
Concentration: 10, 20 μM
Incubation Time: 24 or 48 hours
Result: Caused a decrease in the level of VEGF-R2 protein in HUVEC.

体内研究
(In Vivo)

Z-guggulsterone (oral; 1 mg; 5 times/week) results in a statistically significantly decrease in tumor volume and wet tumor weight[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: Male nude mice (5–6 weeks old) s.c. implanted with DU145 cell-containing Matrigel plugs
Dosage: 1 mg
Administration: Oral; 5 times/week
Result: Resulted in a statistically significantly decrease in tumor volume and wet tumor weight.

分子量

312.45

Formula

C21H28O2
CAS 号

39025-23-5
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 : 10 mg/mL (32.01 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2005 mL 16.0026 mL 32.0051 mL
5 mM 0.6401 mL 3.2005 mL 6.4010 mL
10 mM 0.3201 mL 1.6003 mL 3.2005 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 mg/mL (6.40 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (6.40 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 2.

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

    Solubility: ≥ 1 mg/mL (3.20 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (3.20 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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
*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]. Xiao D, et al. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80.

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

Ginsenoside Rd(Synonyms: 人参皂苷 Rd; Gypenoside VIII)

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。

Ginsenoside Rd (Synonyms: 人参皂苷 Rd; Gypenoside VIII) 纯度: 98.02%

Ginsenoside Rd 抑制 TNFα 诱导的 NF-κB 转录活性，IC50 为 12.05±0.82 μM。Ginsenoside Rd 抑制 COX-2 和 iNOS mRNA 的表达。Ginsenoside Rd 还抑制 Ca2+ 内流。Ginsenoside Rd 抑制CYP2D6，CYP1A2，CYP3A4 和 CYP2C9，IC50 分别为 58.0±4.5 μM，78.4±5.3 μM，81.7±2.6 μM 和 85.1±9.1 μM。

Ginsenoside Rd(Synonyms: 人参皂苷 Rd; Gypenoside VIII)

Ginsenoside Rd Chemical Structure

CAS No. : 52705-93-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1250 In-stock
5 mg ￥700 In-stock
10 mg ￥1200 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Ginsenoside Rd 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Metabolism/Protease Compound Library
  • Neuronal Signaling Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Human Endogenous Metabolite Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Glycoside Compound Library
  • Lipid Compound Library
  • Oxygen Sensing Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Medicine Food Homology Compound Library
  • Terpenoids Library
  • Pyroptosis Compound Library
  • Traditional Chinese Medicine Monomer Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Food-Sourced Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

IC50 & Target

NF-κB

12.05 μM (IC50, in HepG2 cells)

COX-2

 

L-type calcium channel

 

CYP2D6

58 μM (IC50)

CYP1A2

78.4 μM (IC50)

CYP3A4

81.7 μM (IC50)

CYP2C9

85.1 μM (IC50)

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Ginsenoside Rd is one of the most abundant ingredients of Panax ginseng. Ginsenoside Rd significantly inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 in HepG2 cells. Ginsenoside Rd also inhibits expression of COX-2 and iNOS mRNA and iNOS promoter activity in a dose-dependent manner. To determine nontoxic concentrations, HepG2 cells are treated with various concentrations (0.1, 1, and 10 μM) of compounds (e.g., Ginsenoside Rd) and cell viability is measured using an MTS assay. No compounds are significantly cytotoxic at up to 10 μM, indicating that NF-κB inhibition is not due to cell toxicity[1]. Ginsenoside Rd is one of the most abundant ingredients of Panax ginseng, protects the heart via multiple mechanisms including the inhibition of Ca2+ influx. Ginsenoside Rd reduces ICa,L peak amplitude in a concentration-dependent manner (IC50=32.4±7.1 μM)[2]. Ginsenoside Rd exhibits an inhibition against the activity of CYP2D6 in human liver microsomes with an IC50 of 58.0±4.5 μM, a weak inhibition against the activity of CYP1A2, CYP3A4, and CYP2C9 in human liver microsomes with IC50s of 78.4±5.3, 81.7±2.6, and 85.1±9.1, respectively, and an even weaker inhibition against the activity of CYP2A6 in human liver microsomes with an IC50 value of more than 100 μM[4].

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)

Ginsenosides Rd is a major compound isolated from Gynostemma pentaphyllum that holistically improves gut microenvironment and induces anti-polyposis in ApcMin/+ mice. Six-weeks-old mice are subjected to Ginsenoside Rd treatment, before the appearance of the intestinal polyps. All the mice are monitored for food intake, water consumption, and weight changes. Throughout the experiment, no Rb3/ Ginsenoside Rd-associated weight loss in mice is observed. In addition, none of the treated mice show variations in food and water consumption. Whereas, the number and size of the polyps are effectively reduced by Ginsenoside Rd treatments[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.
分子量

947.15

Formula

C48H82O18
CAS 号

52705-93-8
中文名称

人参皂苷 Rd
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 (105.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0558 mL 5.2790 mL 10.5580 mL
5 mM 0.2112 mL 1.0558 mL 2.1116 mL
10 mM 0.1056 mL 0.5279 mL 1.0558 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 (2.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.64 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 (2.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.64 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 (2.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.64 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]. Song SB, et al. Inhibition of TNF-α-mediated NF-κB Transcriptional Activity in HepG2 Cells by Dammarane-type Saponins from Panax ginseng Leaves. J Ginseng Res. 2012 Apr;36(2):146-52.

    [2]. Liu Y, et al. Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes. Toxicol Sci. 2006 Jun;91(2):356-64.

    [3]. Lu C, et al. Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes. J Ginseng Res. 2015 Apr;39(2):169-77.

    [4]. Huang G, et al. Ginsenosides Rb3 and Rd reduce polyps formation while reinstate the dysbiotic gut microbiota and the intestinal microenvironment in ApcMin/+ mice. Sci Rep. 2017 Oct 2;7(1):12552.
Cell Assay
[1]

An MTS assay is used to analyze the effects of the compounds on cell viability. HepG2 cells are cultured overnight in a 96-well plate (1×104 cells/well). Cell viability is assessed after adding the compounds (e.g., Ginsenoside Rd; 0.1, 1, and 10 μM) for 24 h. The number of viable cells is determined by the A490nm of the dissolved formazan product, after addition of MTS for 30 min[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
[3]

Mice[3]
Heterozygous male ApcMin/+ (C57BL/6J-ApcMin/+) mice are used. Total 32 male ApcMin/+ mice (aged 6 weeks) are divided into three groups; 10 mice in the control group and 22 mice equally divided for Rb3 and Rd treatments. The mice are daily gavage with a single dose of Ginsenoside Rb3 or Ginsenoside Rd at 20 mg/kg, or solvent control. The treatments are carried out for 8 consecutive weeks.

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]. Song SB, et al. Inhibition of TNF-α-mediated NF-κB Transcriptional Activity in HepG2 Cells by Dammarane-type Saponins from Panax ginseng Leaves. J Ginseng Res. 2012 Apr;36(2):146-52.

    [2]. Liu Y, et al. Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes. Toxicol Sci. 2006 Jun;91(2):356-64.

    [3]. Lu C, et al. Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes. J Ginseng Res. 2015 Apr;39(2):169-77.

    [4]. Huang G, et al. Ginsenosides Rb3 and Rd reduce polyps formation while reinstate the dysbiotic gut microbiota and the intestinal microenvironment in ApcMin/+ mice. Sci Rep. 2017 Oct 2;7(1):12552.

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

AT9283

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。

AT9283  纯度: 99.70%

AT9283 是一种多靶点激酶抑制剂，有效抑制 Aurora A/B，JAK2/3，Abl (T315I)，和 Flt3 (IC50 值范围为 1-30 nM)。AT9283 抑制多种实体瘤在体内外的生长和存活。

AT9283

AT9283 Chemical Structure

CAS No. : 896466-04-9

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 ￥923 In-stock
2 mg ￥770 In-stock
5 mg ￥1100 In-stock
10 mg ￥1750 In-stock
50 mg ￥5675 In-stock
100 mg ￥9360 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AT9283 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-COVID-19 Compound Library
  • Cytoskeleton Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo[1][2].

IC50 & Target[1]

Aurora A

3 nM (IC50)

Aurora B

3 nM (IC50)

JAK3

1.1 nM (IC50)

JAK2

1.2 nM (IC50)

ABL(T315I)

4 nM (IC50)

Flt-3

 

体外研究
(In Vitro)

AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation[1].
AT9283 induces apoptosis in a dose and time dependent manner and inhibits cell proliferation with an IC50 < 1 μM in B-NHL cell lines[2].
AT9283 inhibits growth, induces dose dependent cytotoxicity, and inhibits STAT3 signaling pathway in MM cell lines. T9283 inhibits phospho Histone H3 and phospho Aurora A at Thr 288. AT9283 increases G2/M phase and induces apoptosis of MM cells in a time-dependent manner[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.
体内研究
(In Vivo)

In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors (2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice[1].
AT9283 (15 mg/kg) and docetaxel (10 mg/kg) alone has modest anti-tumor activity. T9283 at 20 mg/kg and AT9283 (15 or 20 mg/kg) plus docetaxel (10 mg/kg) demonstrate a statistically significant tumor growth inhibition and enhance survival inmouse xenograft model of mantle cell lymphoma[2].
AT9283 (45 mg/kg, i.p.) inhibits tumor growth in mice. Two cycles of AT9283 45 mg/kg 14 hours after drug administration confirm decreased expression of phospho-Histone H3 and Aurora B in treated animals[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

381.43

Formula

C19H23N7O2
CAS 号

896466-04-9
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 (262.17 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 2.6217 mL 13.1086 mL 26.2171 mL
5 mM 0.5243 mL 2.6217 mL 5.2434 mL
10 mM 0.2622 mL 1.3109 mL 2.6217 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 (6.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.55 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 (6.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.55 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 (6.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.55 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]. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388.

    [2]. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005.

    [3]. Santo L, et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin Cancer Res. 2011 May 15;17(10):3259-71
Cell Assay
[2]

Lymphoma cells are seeded at 8,000 per well in 96-well culture plates and allowed to grow for 24 hr followed by the desired treatment with increasing concentrations of the indicated agents for 4 days. Viable cell densities are determined using a CellTiter 96 Cell Proliferation Assay. The IC50 values are estimated by Calcusyn software.

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
[2]

SCID mice are injected with 1×107 Granta-519 MCL cells subcutaneously into the right hind flank. When tumors reached a volume of appr 60-100 mm3, mice are divided randomly (pair-matched) into six test groups with 12 mice per cohort: control group (saline), AT9283 (15 mg/kg IP Q1D, 5 days a week × 3 weeks) group, AT9283 (20 mg/kg IP Q1D, 5 days a week × 3 weeks) group, docetaxel (10 mg/kg IV Q1W × 3 weeks) group, AT9283 (15 mg/kg IP Q1D, 5 days a week × 3 weeks) + docetaxel (10 mg/kg IV Q1W × 3 weeks) group and AT9283 (20 mg/kg IP Q1D, 5 days a week × 3 weeks) + docetaxel (10 mg/kg IV Q1W × 3 weeks) group. The length (L) and width (W) of the subcutaneous tumors are measured by calipers and the tumor volume (TV) is calculated as: TV=(L × W2)/2. Mice are sacrificed at the end of study and overall survival for each cohort is analyzed by Kaplan–Meier method.

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]. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388.

    [2]. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005.

    [3]. Santo L, et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin Cancer Res. 2011 May 15;17(10):3259-71

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

MKC8866

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。

MKC8866  纯度: 98.49%

MKC8866 是一种水杨醛类似物，有效的选择性 IRE1 RNase 抑制剂，在体外的 IC50 为 0.29 μM。 MKC8866 强烈抑制 Dithiothreitol 诱导的 XBP1s 表达，EC50 为 0.52 μM。MKC8866 抑制无应激 RPMI 8226 细胞，IC50 为 0.14 μM。 MKC8866 抑制乳腺癌细胞中的 IRE1 RNase 导致促肿瘤发生因子减少，同时也能抑制前列腺癌 (PCa) 肿瘤的生长。

MKC8866

MKC8866 Chemical Structure

CAS No. : 1338934-59-0

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 ￥2640 In-stock
5 mg ￥2400 In-stock
10 mg ￥3900 In-stock
25 mg ￥7800 In-stock
50 mg ￥12500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

MKC8866 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Endoplasmic Reticulum Stress Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth[2].

IC50 & Target

IC50: 0.29 μM (IRE1 RNase)[1]
体外研究
(In Vitro)

MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines[2].
MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase[2].
MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells[1].
MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s [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 Proliferation Assay[2]

Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells
Concentration: 20 μM
Incubation Time: For 6 days
Result: Decreased proliferation of all breast cancer cell lines.

Cell Cycle Analysis[2]

Cell Line: MDA-MB-231, MCF7 and SKBR3 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: Reduced the number of cells entering S phase.

Cell Cycle Analysis[1]

Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cells
Concentration: 0.2, 0.5, 1, 5, 10 μM
Incubation Time: 3 days
Result: Suppressed the viability of all four cell lines in a dose-dependent manner.

Cell Cycle Analysis[2]

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 72  hours
Result: Completely blocked NSC 125973-induced expression of XBP1s.

体内研究
(In Vivo)

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal[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 athymic nude mice with MDA-MB-231 tumor[1]
Dosage: 300 mg/kg
Administration: Oral; for 28 days
Result: Reduced tumor regrowth post-NSC 125973 withdrawal.

分子量

361.35

Formula

C18H19NO7
CAS 号

1338934-59-0
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 : 16.67 mg/mL (46.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7674 mL 13.8370 mL 27.6740 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 mL
10 mM 0.2767 mL 1.3837 mL 2.7674 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: ≥ 6.75 mg/mL (18.68 mM); Clear solution

    此方案可获得 ≥ 6.75 mg/mL (18.68 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 67.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 2.

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

    Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (4.62 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

  • 3.

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

    Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (4.62 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
*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]. Sheng X, et al. IRE1α-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10(1):323.

    [2]. Logue SE, et al. Inhibition of IRE1 RNase activity modulates the tumor cell secretome and enhances response to chemotherapy. Nat Commun. 2018 Aug 15;9(1):3267.

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