AZD9496

MCE 国际站：AZD9496

产品活性：AZD9496 是有效,选择性的雌激素受体 (ERα) 拮抗剂，IC₅₀ 为 0.28 nM。AZD9496 是一种口服有效的选择性雌激素受体降解剂 (SERD)

研究领域：Vitamin D Related/Nuclear Receptor

In Vitro: The potency of AZD9496 with IC₅₀ of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC₅₀ of 0.04 nM. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC₅₀=30 μM; glucocorticoid receptor (GR), IC₅₀=9.2 μM; progesterone receptor (PR), IC₅₀=0.54 μM.

In Vivo: Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the ICI 182780 control (P<0.001) but significantly lower than ICI 47699 (P=0.001). AZD9496 is also tested in a long-term estrogen deprived model (LTED), using the HCC-1428 LTED cell line that grows in the absence of estrogen and is thought to best represent a model of aromatase inhibition. AZD9496 shows significant activity, with a dose of 5 mg/kg giving tumor regressions in this model.

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