Thailanstatin A
Based on 2 publication(s) in Google Scholar
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.
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- Pureza: 99.09%
- No. CAS: 1426953-21-0
- Fòrmula: C28H41NO9
- Peso molecular:535.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Thailanstatin A
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
145 nM
Compound: 5
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Cytotoxicity against human BT474 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human BT474 cells after 4 days by MTS/cell proliferation assay
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[PMID: 25098528] |
| DU-145 | GI50 |
1.11 nM
Compound: 1, TST-A
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Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
| HEK293 | IC50 |
0.65 μM
Compound: 1, TST-A
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Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay
Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay
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[PMID: 23517093] |
| HEK-293T | IC50 |
296.2 nM
Compound: 5
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Cytotoxicity against HEK293T cells assessed as inhibition in cell growth
Cytotoxicity against HEK293T cells assessed as inhibition in cell growth
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[PMID: 33974423] |
| MDA-MB-231 | GI50 |
2.58 nM
Compound: 1, TST-A
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Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
| MDA-MB-468 | IC50 |
142 nM
Compound: 5
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Cytotoxicity against human MDA-MB-468 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human MDA-MB-468 cells after 4 days by MTS/cell proliferation assay
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[PMID: 25098528] |
| MES-SA | IC50 |
418.6 nM
Compound: 5
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Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth
Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth
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[PMID: 33974423] |
| MES-SA | IC50 |
419 nM
Compound: 116
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Cytotoxicity against human MES-SA cells
Cytotoxicity against human MES-SA cells
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[PMID: 39068862] |
| MES-SA/Dx5 | IC50 |
>400 nM
Compound: 5
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Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth
Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth
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[PMID: 33974423] |
| NCI-H1975 | IC50 |
320 nM
Compound: 5
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Cytotoxicity against human NCI-H1975 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human NCI-H1975 cells after 4 days by MTS/cell proliferation assay
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[PMID: 25098528] |
| NCI-N87 | IC50 |
59 nM
Compound: 5
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Cytotoxicity against human NCI-N87 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human NCI-N87 cells after 4 days by MTS/cell proliferation assay
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[PMID: 25098528] |
| SK-OV-3 | GI50 |
2.69 nM
Compound: 1, TST-A
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Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay
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[PMID: 23517093] |
Thailanstatin A (TST-A) is a potent antiproliferative natural product, can be discovered from Burkholderia thailandensis MSMB43[2].
Thailanstatin A (DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 cells) exhibits potent antiproliferative activities with GI50s in the single nM range (1.11-2.69 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1426953-21-0
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Appearance Solid
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Peso molecular 535.63
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Fòrmula C28H41NO9
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Cell
2025 Apr 17:S1097-2765(25)00307-7. PMID: 40267921 -
Cell Rep
Transient splicing inhibition causes persistent DNA damage and chemotherapy vulnerability in triple-negative breast cancer. [Abstract]2024 Sep 13;43(9):114751. PMID: 39276346
Solvente y solubilidad
DMSO : 100 mg/mL (186.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8670 mL | 9.3348 mL | 18.6696 mL | 46.6740 mL |
| 5 mM | 0.3734 mL | 1.8670 mL | 3.7339 mL | 9.3348 mL | |
| 10 mM | 0.1867 mL | 0.9335 mL | 1.8670 mL | 4.6674 mL | |
| 15 mM | 0.1245 mL | 0.6223 mL | 1.2446 mL | 3.1116 mL | |
| 20 mM | 0.0933 mL | 0.4667 mL | 0.9335 mL | 2.3337 mL | |
| 25 mM | 0.0747 mL | 0.3734 mL | 0.7468 mL | 1.8670 mL | |
| 30 mM | 0.0622 mL | 0.3112 mL | 0.6223 mL | 1.5558 mL | |
| 40 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1669 mL | |
| 50 mM | 0.0373 mL | 0.1867 mL | 0.3734 mL | 0.9335 mL | |
| 60 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7779 mL | |
| 80 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5834 mL | |
| 100 mM | 0.0187 mL | 0.0933 mL | 0.1867 mL | 0.4667 mL |
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