产品描述
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.
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.
Cas No.
1609105-89-6
分子式
C28H41NO8
分子量
519.635
别名
Thailanstatin D
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years