AZD9496

製品コードS8372 バッチS837201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H25F3N2O2
分子量 442.47 CAS No. 1639042-08-2
Solubility (25°C)* 体外 DMSO 88 mg/mL (198.88 mM)
Ethanol 88 mg/mL (198.88 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
in vitro

AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively[1].
in vivo

AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse.AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I clinical trial[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 cells
濃度 100 nM
反応時間 0, 10, 20, 30, 40, 50 h
実験の流れ

Cells were grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as "heavy" and then switched to grow in media containing unlabeled l-arginine to label newly synthesized protein as "normal" with 0.1% DMSO, 300 nmol/L tamoxifen, 100 nmol/L AZD9496 for the time indicated.
動物実験 動物モデル Sexually immature female Han Wistar rats
投薬量 5 and 25 mg/kg once daily
投与方法 by oral gavage

カスタマーフィードバック

, , Onco Targets Ther, 2017, 10: 4809–4819

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

SCR-6852, an oral and highly brain-penetrating estrogen receptor degrader (SERD), effectively shrinks tumors both in intracranial and subcutaneous ER + breast cancer models [ Breast Cancer Res, 2023, 25(1):96] PubMed: 37580832
SCR-6852, an oral and highly brain-penetrating estrogen receptor degrader (SERD), effectively shrinks tumors both in intracranial and subcutaneous ER + breast cancer models [ Breast Cancer Res, 2023, 25(1):96] PubMed: 37580832
G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. [ Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9] PubMed: 32130619
low dose of kaempferol suppresses the migration and invasion of triple-negative breast cancer cells by downregulating the activities of rhoa and rac1 [Li S Onco Targets Ther, 2017, 10:4809-4819] PubMed: 29042792

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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