M17-B15

Chemical Structure : M17-B15

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货号: PC-20797Not For Human Use, Lab Use Only.

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.

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生物&药学活性

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.
M17-B15 forms direct interactions with the AR LBD in a dose-dependent manner with an equilibrium dissociation constant (KD) of 13.2 uM, does not target the ligand binding pocket (LBP).
M17-B15 inhibits AR dimerization at the cellular level.
M17-B15 reduces the PSA levels of LNCaP cells secreted in the cellular media with IC50 of 0.35 uM.
M17-B15 shows significant inhibitory activities toward the colony formation of LNCaP cells but not 22RV1.
M17-B15 (2.5 mg/kg/week) significantly inhibits tumor volume and weight in mouse xenograft tumor, decreases cell density and number and increase necrotic areas are much better than those of second-generation AR antagonist enzalutamide (Enz, Cat. PC-45932).

物理化学性质&存储条件

分子量	409.38
分子式	C18H14F3N3O3S
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	O=C(C1=C(C)OC(C2=CC=CC(C(F)(F)F)=C2)=C1)NC3=NC(CC(C)=O)=NS3

参考文献

1. Weitao Fu , et al. ACS Cent Sci. 2023 Mar 8;9(4):675-684.

M17-B15

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M17-B15

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