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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[1]. | [in vivo]
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.
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| [References]
[1] Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130. DOI:10.1002/ijc.30893 |
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