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Chemical Structure : M17-B15
Catalog No.: 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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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).
| M.Wt | 409.38 | |
| Formula | C18H14F3N3O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Weitao Fu , et al. ACS Cent Sci. 2023 Mar 8;9(4):675-684.
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