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Chemical Structure : AZ3137
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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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.
| M.Wt | 783.90 | |
| Formula | C43H48F3N7O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bagal SK, et al. J Med Chem. 2024 Jul 25;67(14):11732-11750.
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