2. Antibody-drug Conjugate/ADC Related
  3. ADC Payload
  4. Thailanstatin A

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.

For research use only. We do not sell to patients.

Thailanstatin A

Thailanstatin A Chemical Structure

CAS No. : 1426953-21-0

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Based on 2 publication(s) in Google Scholar

Thailanstatin A Related Antibodies

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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].

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]
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]
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.

Thailanstatin A Related Antibodies
Molecular Weight

535.63

Formula

C28H41NO9
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8670 mL 9.3348 mL 18.6696 mL
5 mM 0.3734 mL 1.8670 mL 3.7339 mL
View the 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.71%

SDS (251 KB)

COA (248 KB) HNMR (546 KB) RP-HPLC (260 KB) LCMS (119 KB)

Handling Instructions (2659 KB)
References

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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Thailanstatin A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Thailanstatin A1426953-21-0ADC PayloadADC CytotoxinSF3bsubunitspliceosomeantiproliferativenaturalADClinkerRNAInhibitorinhibitorinhibit

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