Thailanstatin C

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。

Thailanstatin C 

Thailanstatin C 是一种 pre-mRNA 剪接 (pre-mRNA splicing) 抑制剂 (IC50= 6.84 μM),也是一种抗增殖剂。

Thailanstatin C

Thailanstatin C Chemical Structure

CAS No. : 1426953-24-3

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

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生物活性

Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43[1].

体外研究
(In Vitro)

Thailanstatin C inhibits human cancer cell lines with IC50s of 2.98-8.82 nM for DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 cells[1].

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

分子量

600.14

Formula

C30H46ClNO9

CAS 号

1426953-24-3

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]. Liu X, et al. Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43. J Nat Prod. 2013;76(4):685-693.

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

Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[1].

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

Cell Viability Assay[1]

Cell Line: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1].

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

Animal Model: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Thailanstatin C

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。

Thailanstatin C 

Thailanstatin C 是一种 pre-mRNA 剪接 (pre-mRNA splicing) 抑制剂 (IC50= 6.84 μM),也是一种抗增殖剂。

Thailanstatin C

Thailanstatin C Chemical Structure

CAS No. : 1426953-24-3

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

Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43[1].

体外研究
(In Vitro)

Thailanstatin C inhibits human cancer cell lines with IC50s of 2.98-8.82 nM for DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 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.

分子量

600.14

Formula

C30H46ClNO9

CAS 号

1426953-24-3

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]. Liu X, et al. Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43. J Nat Prod. 2013;76(4):685-693.

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

Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[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: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[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: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Thailanstatin C

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。

Thailanstatin C 

Thailanstatin C 是一种 pre-mRNA 剪接 (pre-mRNA splicing) 抑制剂 (IC50= 6.84 μM),也是一种抗增殖剂。

Thailanstatin C

Thailanstatin C Chemical Structure

CAS No. : 1426953-24-3

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

Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43[1].

体外研究
(In Vitro)

Thailanstatin C inhibits human cancer cell lines with IC50s of 2.98-8.82 nM for DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 cells[1].

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

分子量

600.14

Formula

C30H46ClNO9

CAS 号

1426953-24-3

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]. Liu X, et al. Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43. J Nat Prod. 2013;76(4):685-693.

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

Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[1].

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

Cell Viability Assay[1]

Cell Line: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1].

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

Animal Model: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Thailanstatin A(Synonyms: 泰兰斯他汀A)

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。

Thailanstatin A (Synonyms: 泰兰斯他汀A) 纯度: ≥98.0%

Thailanstatin A 是一种有效的真核 RNA 剪接 (RNA splicing) 抑制剂 (IC50=650 nM)。Thailanstatin A 通过非共价结合到剪接体的 U2 snRNA 亚复合物的 SF3b 亚单位发挥作用,并且对多种癌细胞系显示低 nM 到亚 nM 的 IC50 值。Thailanstatin A 与 Trastuzumab 上的赖氨酸结合,可产生“无连接子 (linker-less)” ADC。

Thailanstatin A(Synonyms: 泰兰斯他汀A)

Thailanstatin A Chemical Structure

CAS No. : 1426953-21-0

规格 价格 是否有货 数量
1 mg ¥2800 In-stock
5 mg ¥8500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Thailanstatin A 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library

生物活性

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC[1][2][3].

体外研究
(In Vitro)

Thailanstatin A (TST-A) is a potent antiproliferative natural product discovered by our group from Burkholderia thailandensis MSMB43[2].
Thailanstatin A (DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 cells) exhibits potent antiproliferative activities with GI50s in the single nM range (1.11-2.69 nM)[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

535.63

Formula

C28H41NO9

CAS 号

1426953-21-0

中文名称

泰兰斯他汀A

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 : 250 mg/mL (466.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8670 mL 9.3348 mL 18.6696 mL
5 mM 0.3734 mL 1.8670 mL 3.7339 mL
10 mM 0.1867 mL 0.9335 mL 1.8670 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.88 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.88 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 20.8 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]. Puthenveetil S, et al. Natural Product Splicing Inhibitors: A New Class of Antibody-Drug Conjugate (ADC) Payloads. Bioconjug Chem. 2016;27(8):1880-1888.

    [2]. Ghosh AK, et al. Enantioselective Synthesis of Thailanstatin A Methyl Ester and Evaluation of in Vitro Splicing Inhibition. J Org Chem. 2018;83(9):5187-5198.

    [3]. Liu X, et al. Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43. J Nat Prod. 2013;76(4):685-693.

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