ERα degrader-2
目录号: PL03272 纯度: ≥99%
ERα degrader-2 是一种选择性雌激素受体降解剂 (SERD),与 ERα (IC50=17.1 nM) 有较强的结合亲和力,具有较好的降解效果(EC50=0.3 nM)。ERα degrader-2 具有良好的药代动力学特性和优良的成药性质,可用于HER 阳性乳腺癌研究。
CAS No. :2235396-63-9
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中文名称
ERα degrader-2
英文名称
ERα degrader-2
英文别名
[1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]-;ERα degrader-2
Cas No.
2235396-63-9
分子式
C29H27F3N2O2
分子量
492.53
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
ERα degrader-2 是一种选择性雌激素受体降解剂 (SERD),与 ERα (IC50=17.1 nM) 有较强的结合亲和力,具有较好的降解效果(EC50=0.3 nM)。ERα degrader-2 具有良好的药代动力学特性和优良的成药性质,可用于HER 阳性乳腺癌研究。
生物活性
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC 50 =17.1 nM), good degradation efficacy (EC 50 =0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent druggability, can be used for HER breast cancer research.
性状
Solid
IC50 & Target[1][2]
ERα 4.6 nM (IC50)
体外研究(In Vitro)
ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice.
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Xiaomeng Zhang, et al. Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer. J Med Chem
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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