Art. -Nr.: HY-129589

Thailanstatin A

2 Cited Publications

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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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Reinheit: 99.09%
CAS. Nr.: 1426953-21-0
Formel: C₂₈H₄₁NO₉
Molecular Weight:535.63

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Thailanstatin A Chemical Structure

CAS. Nr.: 1426953-21-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle ADC Payloads Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-474	IC₅₀	145 nM Compound: 5	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	[PMID: 25098528]
DU-145	GI₅₀	1.11 nM Compound: 1, TST-A	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	[PMID: 23517093]
HEK293	IC₅₀	0.65 μM Compound: 1, TST-A	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	[PMID: 23517093]
HEK-293T	IC₅₀	296.2 nM Compound: 5	Cytotoxicity against HEK293T cells assessed as inhibition in cell growth Cytotoxicity against HEK293T cells assessed as inhibition in cell growth	[PMID: 33974423]
MDA-MB-231	GI₅₀	2.58 nM Compound: 1, TST-A	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	[PMID: 23517093]
MDA-MB-468	IC₅₀	142 nM Compound: 5	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	[PMID: 25098528]
MES-SA	IC₅₀	418.6 nM Compound: 5	Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth	[PMID: 33974423]
MES-SA	IC₅₀	419 nM Compound: 116	Cytotoxicity against human MES-SA cells Cytotoxicity against human MES-SA cells	[PMID: 39068862]
MES-SA/Dx5	IC₅₀	>400 nM Compound: 5	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	[PMID: 33974423]
NCI-H1975	IC₅₀	320 nM Compound: 5	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	[PMID: 25098528]
NCI-N87	IC₅₀	59 nM Compound: 5	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	[PMID: 25098528]
SK-OV-3	GI₅₀	2.69 nM Compound: 1, TST-A	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	[PMID: 23517093]

In Vitro

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

CAS. Nr. 1426953-21-0
Appearance Solid
Molecular Weight 535.63
Formel C₂₈H₄₁NO₉
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Mol Cell

ZBP1 senses spliceosome stress through Z-RNA:DNA hybrid recognition. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8670 mL

9.3348 mL

18.6696 mL

5 mM

0.3734 mL

1.8670 mL

3.7339 mL

10 mM

0.1867 mL

0.9335 mL

1.8670 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Thailanstatin A

2 Cited Publications

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Thailanstatin A

Toxins for Antibody-Drug Conjugate Research Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Thailanstatin A

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Thailanstatin A

Toxins for Antibody-Drug Conjugate Research Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Thailanstatin A

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Thailanstatin A Related Classifications

HY-129589 Related Classifications