Thailanstatin D
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis.
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- CAS. Nr.: 1609105-89-6
- Formel: C28H41NO8
- Molecular Weight:519.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
4.8 nM
Compound: 4
|
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] |
| MDA-MB-468 | IC50 |
3.4 nM
Compound: 4
|
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 |
3.6 nM
Compound: 4
|
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 |
2 nM
Compound: 4
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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
|
[PMID: 25098528] |
Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP, 22RV1 and LN95 cells
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Concentration:0-50 nM
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Incubation Time:4 hours
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Result:The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
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Dosage:300 µg/kg
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Administration:ALZET osmotic pumps; daily for 4 days
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Result:Significantly inhibited the tumor growth.
Chemical Information
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CAS. Nr. 1609105-89-6
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Molecular Weight 519.63
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Formel C28H41NO8
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SMILES
C[C@@H](C[C@H]([C@H](O1)C)NC(/C=C\[C@H](C)OC(C)=O)=O)[C@@H]1C/C=C(C)/C=C/[C@@H]2C[C@@]3(C[C@H](O2)CC(O)=O)CO3
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Structure Classification
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Initial Source
Burkholderia thailandensis
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)