标签归档：silvestrol

Silvestrol aglycone (enantiomer)

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。

Silvestrol aglycone (enantiomer)  纯度: 99.10%

Silvestrol aglycone enantiomer 是 Silvestrol 的糖苷配基对映体，是一种环戊苯并呋喃核酚。

Silvestrol aglycone (enantiomer)

Silvestrol aglycone (enantiomer) Chemical Structure

CAS No. : 1112993-18-6

规格 价格 是否有货 数量
5 mg ￥9500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Silvestrol aglycone (enantiomer) 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Silvestrol aglycone enantiomer is a cyclopenta benzofuran core phenol[1].

分子量

478.49

Formula

C27H26O8
CAS 号

1112993-18-6
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 : ≥ 114 mg/mL (238.25 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 2.0899 mL 10.4495 mL 20.8991 mL
5 mM 0.4180 mL 2.0899 mL 4.1798 mL
10 mM 0.2090 mL 1.0450 mL 2.0899 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: ≥ 7.5 mg/mL (15.67 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.67 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 7.5 mg/mL (15.67 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.67 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 7.5 mg/mL (15.67 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.67 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 75.0 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]. Adams TE, et al. Total synthesis of the potent anticancer Aglaia metabolites (-)-silvestrol and (-)-episilvestrol and the active analogue (-)-4′-desmethoxyepisilvestrol. J Am Chem Soc. 2009 Feb 4;131(4):1607-16.

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

Silvestrol(Synonyms: (-)-Silvestrol)

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。

Silvestrol (Synonyms: (-)-Silvestrol) 纯度: 98.11%

Silvestrol 是从 Aglaia foveolata 的果实和枝条中分离的真核翻译起始因子 (eIF4A) 抑制剂。Silvestrol 诱导细胞自噬以及 caspase 介导的细胞凋亡。

Silvestrol(Synonyms: (-)-Silvestrol)

Silvestrol Chemical Structure

CAS No. : 697235-38-4

规格 价格 是否有货 数量
1 mg ￥9900 In-stock
2 mg ￥16500 In-stock
5 mg ￥32000 In-stock
10 mg ￥45000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Silvestrol 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis[1][2][3].

IC50 & Target

eIF4A[1]
体外研究
(In Vitro)

Silvestrol is a specific eIF4A-targeting translation inhibitor. Silvestrol exhibits significant cytotoxic activity against many human cancer cell lines, such as lung, prostate, and breast cancer with IC50 values ranging from 1 to 7 nM[1].
Silvestrol significantly reduces the number of LNCaP cell colonies. Silvestrol (30 nM, 120 nM) induces apoptosis in LNCaP cells, through the mitochondrial pathway. Apaf-1, Caspase-2, caspase-9, and caspase-10 are involved in Silvestrol-induced apoptosis but caspase-3 and 7 are not[2].
Silvestrol induces caspase-3 activation and apoptotic cell death in a time- and dose-dependent manner. Silvestrol-mediated cell death is attenuated in ATG7-null mouse embryonic fibroblasts (MEFs) lacking a functional autophagy protein[3].
Silvestrol (50 nM) exerts an immediate inhibitory effect and causes near-static cell index compared with the control cells. Silvestrol (6.25 nM) enhances proliferation more than the vehicle control-treated cells, whereas a higher concentration of Silvestrol (50 nM) can inhibit cell proliferation. Silvestrol and episilvestrol display synergistic effects in combination with CDDP[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)

Silvestrol (1.5 mg/kg, i.p.) does not adversely affect production of human IgG by xenografted B-lymphocytes in mice. Silvestrol significantly prolongs survival compared to vehicle. There is no such lymphocyte infiltration detected in the spleens of any of the Silvestrol-treated mice, and nor do these animals exhibit any other obvious signs of lymphoma upon necropsy[5].

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

654.66

Formula

C34H38O13
CAS 号

697235-38-4
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 : ≥ 6.6 mg/mL (10.08 mM)

H2O : < 0.1 mg/mL (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5275 mL 7.6376 mL 15.2751 mL
5 mM 0.3055 mL 1.5275 mL 3.0550 mL
10 mM 0.1528 mL 0.7638 mL 1.5275 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:
  • 1.

    Silvestrol is prepared in 5.2% Tween 80 5.2% PEG 400[6].

  • 2.

    Silvestrol is dissolved in 20%(w/v) 2-hydroxyproply beta-cyclodextrin vehicle at a concentration of 125 μg/mL and injected into mice i.p.[7].

  • 3.

    Silvestrol is formulated in 30% 2-hydroxypropyl-β-cyclodextrin[8].
参考文献

  • [1]. Chambers JM, et al. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II. Org Lett. 2013 Mar 15;15(6):1406-9.

    [2]. Kim S, et al. Silvestrol, a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7. Anticancer Res. 2007 Jul-Aug;27(4B):2175-83.

    [3]. Chen WL, et al. Silvestrol induces early autophagy and apoptosis in human melanoma cells. BMC Cancer. 2016 Jan 13;16:17.

    [4]. Daker M, et al. Inhibition of nasopharyngeal carcinoma cell proliferation and synergism of CDDP with silvestrol and episilvestrol isolated from Aglaia stellatopilosa. Exp Ther Med. 2016 Jun;11(6):2117-2126.

    [5]. Patton JT, et al. The translation inhibitor silvestrol exhibits direct anti-tumor activity while preserving innate and adaptive immunity against EBV-driven lymphoproliferative disease. Oncotarget. 2015 Feb 20;6(5):2693-708.

    [6]. Wolfe AL, et al. RNA G-quadruplexes cause eIF4A-dependent oncogene translation in cancer. Nature. 2014 Sep 4;513(7516):65-70.

    [7]. Wiegering A, et al. Targeting Translation Initiation Bypasses Signaling Crosstalk Mechanisms That Maintain High MYC Levels in Colorectal Cancer. Cancer Discov. 2015 Jul;5(7):768-781.

    [8]. Todt D, et al. The natural compound silvestrol inhibits hepatitis E virus (HEV) replication in vitro and in vivo. Antiviral Res. 2018 Sep;157:151-158.
Cell Assay
[2]

The cells are seeded at a density of 7×104 cells/mL in 100-mm culture dishes and are treated with 30 nM or 120 nM concentrations of Silvestrol for 24 h[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]

Mice[5]
Peripheral blood mononuclear cells (PBMC) are injected intraperitoneally (IP) into SCID mice depleted of murine natural killer (NK) cells by pretreatment (plus weekly re-treatment) with anti-asialo (GM1). Engraftment is confirmed by hu-IgG ELISA. Treatments with vehicle (30% hydroxypropyl-β-cyclodextrin) or Silvestrol (1.5 mg/kg every 48 hr IP) begin 2 weeks post-engraftment[5].

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]. Chambers JM, et al. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II. Org Lett. 2013 Mar 15;15(6):1406-9.

    [2]. Kim S, et al. Silvestrol, a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7. Anticancer Res. 2007 Jul-Aug;27(4B):2175-83.

    [3]. Chen WL, et al. Silvestrol induces early autophagy and apoptosis in human melanoma cells. BMC Cancer. 2016 Jan 13;16:17.

    [4]. Daker M, et al. Inhibition of nasopharyngeal carcinoma cell proliferation and synergism of CDDP with silvestrol and episilvestrol isolated from Aglaia stellatopilosa. Exp Ther Med. 2016 Jun;11(6):2117-2126.

    [5]. Patton JT, et al. The translation inhibitor silvestrol exhibits direct anti-tumor activity while preserving innate and adaptive immunity against EBV-driven lymphoproliferative disease. Oncotarget. 2015 Feb 20;6(5):2693-708.

    [6]. Wolfe AL, et al. RNA G-quadruplexes cause eIF4A-dependent oncogene translation in cancer. Nature. 2014 Sep 4;513(7516):65-70.

    [7]. Wiegering A, et al. Targeting Translation Initiation Bypasses Signaling Crosstalk Mechanisms That Maintain High MYC Levels in Colorectal Cancer. Cancer Discov. 2015 Jul;5(7):768-781.

    [8]. Todt D, et al. The natural compound silvestrol inhibits hepatitis E virus (HEV) replication in vitro and in vivo. Antiviral Res. 2018 Sep;157:151-158.

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

Silvestrol aglycone

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。

Silvestrol aglycone  纯度: 99.70%

Silvestrol aglycone 是 Silvestrol 的类似物，能够抑制癌细胞蛋白翻译起始，对蛋白翻译荧光素酶报告基因 yc-LUC 和 tub-LUC 的 EC50 值分别为 10 和 200 nM。具有抗癌作用。

Silvestrol aglycone

Silvestrol aglycone Chemical Structure

CAS No. : 960365-65-5

规格 价格 是否有货 数量
5 mg ￥9500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Silvestrol aglycone 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity[1].

体外研究
(In Vitro)

Silvestrol aglycone (Compound 4) inhibits the proliferation of MDA-MB-231 cells with an E50 of 20 ± 10 nM after 72 h[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

478.49

Formula

C27H26O8
CAS 号

960365-65-5
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 : ≥ 106 mg/mL (221.53 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 2.0899 mL 10.4495 mL 20.8991 mL
5 mM 0.4180 mL 2.0899 mL 4.1798 mL
10 mM 0.2090 mL 1.0450 mL 2.0899 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: ≥ 7.5 mg/mL (15.67 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.67 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 7.5 mg/mL (15.67 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.67 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 75.0 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]. Liu T, et al. Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors. J Med Chem. 2012 Oct 25;55(20):8859-78.

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