Thailanstatin A

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].

Product Specifications

CAS Number

[1426953-21-0]

UNSPSC

12352203

Target

ADC Payload

Type

ADC Related

Related Pathways

Antibody-drug Conjugate/ADC Related

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/thailanstatin-a.html

Purity

99.71

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(O)C[C@@H](O[C@H](/C=C/C(C)=C/C[C@H]1[C@@H](C)C[C@@H](NC(/C=C\[C@@H](OC(C)=O)C)=O)[C@@H](C)O1)[C@H]2O)C[C@]32CO3

Molecular Formula

C28H41NO9

Molecular Weight

535.63

References & Citations

[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.