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.
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 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.
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.
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 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.
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.
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 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.
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 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.
[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.