计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,充氩,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AZD9496 maleate is a potent and selective estrogen receptor ( ERα ) antagonist with IC 50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
In Vitro
The potency of AZD9496 with IC 50 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 EC 50 of 0.04 nM. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC 50 =30 μM; glucocorticoid receptor (GR), IC 50 =9.2 μM; progesterone receptor (PR), IC 50 =0.54 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 0.28 nM (ERα antagonism), 0.14 nM (ERα downregulation), 0.82 nM (ERα binding)
规格
别名
AZD9496 马来酸盐
规格或纯度
10mM in DMSO
英文名称
AZD9496 maleate
生化机理
AZD9496 马来酸盐是一种强效的选择性雌激素受体（ERα）拮抗剂，IC 50 为 0.28 nM。AZD9496 马来酸盐是一种口服生物活性选择性雌激素受体降解剂（SERD）。
储存条件
避光,充氩,-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
分子量
558.55
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
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