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Amcenestrant

(Synonyms: SAR439859)

目录号: PL03328 纯度: ≥99%

SAR439859 (compound 43d) 是一种具有口服活性，非甾体和选择性雌激素受体降解剂 (SERD)。SAR439859 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC50 为 0.2 nM。SAR439859 可在 ER⁺ 乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

CAS No. :2114339-57-8

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中文名称	Amcenestrant
英文名称	Amcenestrant
英文别名	SAR439859;TBF1NHY02O;6-(2,4-dichlorophenyl)-5-[4-[(3~{S})-1-(3-fluoranylpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7~{H}-benzo[7]annulene-2-carboxylic acid;Amcenestrant;Amcenestrant [INN];US9714221, Example 51;BDBM263716;Q66885452;8-(2,4-Dichlorophenyl)-9-(4-(((3S)-1-(3-fluoropropyl)-3-pyrrolidinyl)oxy)phenyl)-6,7-dihydro-5H-benzocycloheptene-3-carboxylic acid;L5B;6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3;Unii-tbf1nhy02O;(S)-8-(2,4-Dichlorophenyl)-9-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)oxy)phenyl)-6,7-dihydro-5H-benzo[7]annulene-3-carboxylic acid;6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid;8-(2,4-Dichlorophenyl)-9-[4-[[(3S)-1-(3-fluoropropyl)-3-pyrrolidinyl]oxy]phenyl]-6,7-dihydro-5H-benzocycloheptene-3-carboxylic acid;6-(2,4-dichlorophenyl)-5-[4-[(3~{S}
Cas No.	2114339-57-8
分子式	C₃₁H₃₀Cl₂FNO₃
分子量	554.48
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	SAR439859 (compound 43d) 是一种具有口服活性，非甾体和选择性雌激素受体降解剂 (SERD)。SAR439859 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC50 为 0.2 nM。SAR439859 可在 ER⁺ 乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

产品详情

SAR439859 (compound 43d) 是一种具有口服活性，非甾体和选择性雌激素受体降解剂 (SERD)。SAR439859 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC₅₀ 为 0.2 nM。SAR439859 可在 ER⁺ 乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

生物活性

SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC 50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER breast cancer.

性状

Solid

IC50 & Target[1][2]

ERα 0.2 nM (EC50)

体外研究(In Vitro)

SAR439859 (compound 43d) induces strong in vivo antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID.
SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows a low to moderate clearance in the three animal species tested (0.03-1.92 L/h?kg), low to moderate volume of distribution (V ss =0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T 1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog).
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

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. El-Ahmad Y, et al. Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Est
[2]. Monsif Bouaboula, et al. Abstract 943: SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust antitumor efficacy and limited cross-resistance in ER breast cancer.

溶解度数据	In Vitro: DMSO : 83.33 mg/mL (150.28 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

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。

Amcenestrant

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