Chemical Structure : M17-B15
CAS No.:
708291-86-5
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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409.38
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Formula
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C18H14F3N3O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(C1=C(C)OC(C2=CC=CC(C(F)(F)F)=C2)=C1)NC3=NC(CC(C)=O)=NS3
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References
1. Weitao Fu , et al. ACS Cent Sci. 2023 Mar 8;9(4):675-684.
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