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Thailanstatin A

Catalog No. T38889   CAS 1426953-21-0

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.

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Thailanstatin A Chemical Structure
Thailanstatin A, CAS 1426953-21-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 197.00
2 mg In stock $ 327.00
5 mg In stock $ 579.00
10 mg In stock $ 829.00
25 mg In stock $ 1,270.00
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Purity: 99.35%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
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) shows potent antiproliferative activities with GI 50 s in the single nM range (1.11-2.69 nM) [3].
Molecular Weight 535.63
Formula C28H41NO9
CAS No. 1426953-21-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 245 mg/mL (457.41 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Inhibitor Library Bioactive Compound Library

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Keywords

Thailanstatin A 1426953-21-0 ADC Payload natural Inhibitor inhibit SF3b subunit antiproliferative spliceosome ADC ADC Cytotoxin RNA linker inhibitor

 

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