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Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.
Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | 询价 | 期货 |
产品描述 | Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis. |
体外活性 | Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[1]. Cell Viability Assay[1]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. |
体内活性 | Thailanstatin D (300 μg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1]. 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. |
分子量 | 519.635 |
分子式 | C28H41NO8 |
CAS No. | 1609105-89-6 |
密度 | 1.19 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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