产品描述

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing ( IC 50 =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 IC 50 s 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] .

体外活性

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 GI 50 s in the single nM range (1.11-2.69 nM) [3] .

别名

泰兰斯他汀A

分子量

535.63

分子式

C28H41NO9

CAS No.

1426953-21-0

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 245 mg/mL (457.41 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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.

Note

For research use only .