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.
For research use only. We do not sell to patients.
- CAS No.: 1609105-89-6
- Formula: C28H41NO8
- Molecular Weight:519.63
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
|
Cell Line
|
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
|
[PMID: 25098528] |
| NCI-N87 | IC50 |
2 nM
Compound: 4
|
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.
-
Cell Line:VCaP, 22RV1 and LN95 cells
-
Concentration:0-50 nM
-
Incubation Time:4 hours
-
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.
-
Animal Model:NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
-
Dosage:300 µg/kg
-
Administration:ALZET osmotic pumps; daily for 4 days
-
Result:Significantly inhibited the tumor growth.
Chemical Information
-
CAS No. 1609105-89-6
-
Molecular Weight 519.63
-
Formula C28H41NO8
-
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
-
Structure Classification
-
Initial Source
Burkholderia thailandensis
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)