AZ3137 | AR degrader | Probechem Biochemicals

Chemical Structure : AZ3137

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AZ3137 (AZ'3137)

货号: PC-22824Not For Human Use, Lab Use Only.

AZ3137 (AZ′3137) a potent, selective, orally bioavailable androgen aeceptor (AR) PROTAC degrader with DC50 of 22 nM and 92 nM for LNCaP cells expressing WT AR and AR T878A/L702H respectively.

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生物&药学活性

AZ3137 (AZ′3137) a potent, selective, orally bioavailable androgen aeceptor (AR) PROTAC degrader with DC50 of 22 nM and 92 nM for LNCaP cells expressing WT AR and AR T878A/L702H respectively.
AZ′3137 degrades amplified and mutant AR, inhibits the expression of AR target genes with similar potency and to a similar extent as enzalutamide in LNCaP cells.
AZ′3137 inhibits the proliferation of LNCaPs with a GI50 value of 74 nM, which is equivalent to or better than three AR antagonists, enzalutamide, apalutamide, and darolutamide.
AZ′3137 (30 mg/kg for 10 days) degrades AR and inhibits tumor growth in C4–2 model.

物理化学性质&存储条件

分子量	783.90
分子式	C43H48F3N7O4
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	4-(4-{4-[4-({4-[2-(2,6-Dioxopiperidin-3-yl)-7-methoxy-1-oxo-2,3-dihydro-1H-isoindol-5-yl]-piperazin-1-yl}methyl)piperidin-1-yl]phenyl}piperidin-1-yl)-2-(trifluoromethyl)benzonitrile

参考文献

1. Bagal SK, et al. J Med Chem. 2024 Jul 25;67(14):11732-11750.

AZ3137 (AZ'3137)

生物&药学活性

物理化学性质&存储条件

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AZ3137 (AZ'3137)

生物&药学活性

物理化学性质&存储条件

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