MTX-23

Chemical Structure : MTX-23

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货号: PC-21124Not For Human Use, Lab Use Only.

MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively.

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生物&药学活性

MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively.
MTX-23 simultaneously binds AR's DNA binding domain (DBD) and the Von Hippel-Lindau (VHL) E3 ubiquitin ligase.
MTX-23 inhibits prostate cancer cellular proliferation and increased apoptosis only in androgen-responsive prostate cancer cells.
MTX-23 (1 uM) stimulates apoptosis in 22Rv1 cells, induces poly-ubiquitination of AR-V7 and AR-FL.
MTX-23 is effective against SAT-resistant prostate cancer cell lines, inhibits enzalutamide-resistant prostate cancer growth in mice.

物理化学性质&存储条件

分子量	882.06
分子式	C43H53F2N7O7S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S,4R)-1-[(2S)-2-[5-[[2-[2,3-difluoro-6-(2-morpholinothiazol-4-yl)phenoxy]acetyl]amino]pentanoylamino]-3,3-dimethyl-butanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methylthiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide

参考文献

1. Geun Taek Lee, et al. Mol Cancer Ther. 2021 Mar;20(3):490-499.

MTX-23

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MTX-23

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