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Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $197 | In Stock | |
2 mg | $327 | In Stock | |
5 mg | $579 | In Stock | |
10 mg | $829 | In Stock | |
25 mg | $1,270 | In Stock | |
50 mg | Inquiry | In Stock |
Description | Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as 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 |
Smiles | C[C@H](OC(C)=O)\C=C/C(=O)N[C@@H]1C[C@H](C)[C@H](C\C=C(/C)\C=C\[C@H]2O[C@H](CC(O)=O)C[C@@]3(CO3)[C@@H]2O)O[C@@H]1C |
Relative Density. | 1.23 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 245 mg/mL (457.41 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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