Chemical Structure : AZ3137
CAS No.:
2960179-53-5
AZ3137
(AZ'3137)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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783.90
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Formula
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C43H48F3N7O4
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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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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
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References
1. Bagal SK, et al. J Med Chem. 2024 Jul 25;67(14):11732-11750.
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