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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-Camizestrant
Camizestrant

Chemical Structure : Camizestrant

CAS No.: 2222844-89-3

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Camizestrant (AZD-9833, AZD9833)

货号: PC-72606Not For Human Use, Lab Use Only.

AZD9833 (Camizestrant) is an orally bioavailable, highly potent, next-generation selective estrogen receptor degrader (SERD) and antagonist with both EC50 of <1 nM (ERα receptor) in MCF7 cells.

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5 mg ￥2780 In stock
10 mg ￥3980 In stock
25 mg ￥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD9833 (Camizestrant) is an orally bioavailable, highly potent, next-generation selective estrogen receptor degrader (SERD) and antagonist with both EC50 of <1 nM (ERα receptor) in MCF7 cells.
AZD9833 demonstrated to be a highly potent SERD that showed a pharmacological profile comparable to fulvestrant in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines.
In contrast to AZD9496, AZD9833 does not cause ER agonism in the endometrial carcinoma cell line Ishikawa in vitro and does not cause an increase in the thickness of the endometrium in juvenile rats.
AZD9833 completely suppresses tumor growth in several patient-derived and cell line xenograft models, including models with clinically relevant ESR1 mutations.

物理化学性质&存储条件

分子量 476.524
分子式 C24H28F4N6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

200 mM in DMSO (95.3 mg/mL)
Chemical Name/SMILES

N-[1-(3-fluoropropyl)azetidin-3-yl]-6-[(6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl]pyridin-3-amine

参考文献

1. Bamberg K, et al. PLoS One. 2018 Feb 23;13(2):e0193380.

2. Granberg KL, et al. J Med Chem. 2019 Feb 14;62(3):1385-1406.

3. Whittaker A, et al. Clin Transl Sci. 2020 Mar;13(2):275-283.

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