Giredestrant (Synonyms: GDC-9545; RG6171)
目录号: PL01776 纯度: ≥99%
Giredestrant (GDC-9545) 是一种非甾体雌激素受体 (ER) 配体,口服有效的,选择性 ER 拮抗剂。Giredestrant 可以在 ER 配体结合域内与雌二醇 (Estradiol) 竞争结合并诱导构象变化。Giredestrant 具有抗肿瘤活性。
CAS No. :1953133-47-5
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中文名称
Giredestrant
英文名称
Giredestrant
英文别名
Giredestrant;28P3DU6DB3;Giredestrant [INN];GQCXHIKRWBIQMD-AKJBCIBTSA-N;3-((1R,3R)-1-(2,6-Difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido(3,4-b)indol-2-yl)-2,2-difluoropropan-1-ol;3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoro-propan-1-ol;2H-Pyrido(3,4-b)indole-2-propanol, 1-(2,6-difluoro-4;GDC-9545
Cas No.
1953133-47-5
分子式
C27H31F5N4O
分子量
522.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Giredestrant (GDC-9545) 是一种非甾体雌激素受体 (ER) 配体,口服有效的,选择性 ER 拮抗剂。Giredestrant 可以在 ER 配体结合域内与雌二醇 (Estradiol) 竞争结合并诱导构象变化。Giredestrant 具有抗肿瘤活性。
生物活性
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
性状
Solid
IC50 & Target[1][2]
ER
体外研究(In Vitro)
Giredestrant (GDC-9545) is a novel ER antagonist that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile. 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]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes
溶解度数据
In Vitro: DMSO : 50 mg/mL (95.68 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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