您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > SAR439859(Amcenestrant)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
SAR439859(Amcenestrant)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SAR439859(Amcenestrant)图片
CAS NO:2114339-57-8
包装:5mg, 10mg
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
SAR-439859
Amcenestrant
产品介绍

生物活性

SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation. SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth.

In vivo treatment with SAR439859 demonstrates significant tumor regression in ER+ breast cancer models, including MCF7-ESR1 wild-type and mutant-Y537S mouse tumors, and HCI013, a patient-derived tamoxifen-resistant xenograft tumor. SAR439859 (2.5-25 mg/kg; orally twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID.


化学数据

分子量554.48
分子式C31H30Cl2FNO3
CAS号2114339-57-8
纯度>99%
溶解性(25°C)DMSO 80 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系LCC2 cells, MCF7 cells
方法Trypsinized cells are dispensed into 384-well plates in IMEM (supplemented with 5% FBS) and after overnight incubation cells are treated with SAR439859 for the times indicated. Cell viability is assessed using CellTiter-Glo according to the manufacturer’s protocol and relative luminescence units (RLU) are measured using an Envision Multilabel Reader. The RLUs of the treated samples are normalized to that of the untreated samples and cell viability is expressed as a percentage of the value of the untreated cells.
浓度0.01-1000 nM
处理时间7 days, 4 hours

动物实验
动物模型Nu/nu mouse with MCF7 tumor xenograft model
配制solution (0.6 mg/mL) in glycofurol/PS80/G5 (10%/5%/85%) and solution (1 mg/mL) in labrasol/solutol/G5 (20%/5%/75%)
剂量2.5, 5, 12.5, 25 mg/kg
给药处理Orally; twice daily for 30 days

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.8035 mL9.0175 mL18.0349 mL
5 mM0.3607 mL1.8035 mL3.607 mL
10 mM0.1803 mL0.9017 mL1.8035 mL