Thailanstatin D

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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

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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.

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