Thailanstatin A 是真核 RNA 剪接抑制剂，IC50为650 nM，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。Thailanstatin A对多种癌细胞系的抑制显示 nM级别的 IC50。它与 Trastuzumab 上的赖氨酸结合，可产生“无连接子” ADC。

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 =650 nM). Thailanstatin A inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC 50 s against . Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.

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) shows potent antiproliferative activities with GI 50 s in the single nM range (1.11-2.69 nM) [3].

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C28H41NO9

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DMSO:245 mg/mL (457.41 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years