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Thailanstatin A

$250$780

Products Details

Product Description

– 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].

Web ID

– HY-129589

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-programmed cell death

Molecular Formula

– C28H41NO9

References

– [1]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.|[2]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.|[3]Puthenveetil S, et al. Natural Product Splicing Inhibitors: A New Class of Antibody-Drug Conjugate (ADC) Payloads. Bioconjug Chem. 2016;27(8):1880-1888.

CAS Number

– 1426953-21-0

Molecular Weight

– 535.63

Compound Purity

– 98.51

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 250 mg/mL (ultrasonic)

Target

– ADC Cytotoxin

Pathway

– Antibody-drug Conjugate/ADC Related

Product type

– ADC Related

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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