AZD3463

製品コードS7106 バッチS710601

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

C24H25ClN6O
分子量 448.95 CAS No. 1356962-20-3
Solubility (25°C)* 体外 DMSO 6 mg/mL (13.36 mM)
Water Insoluble
Ethanol 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 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
in vitro AZD3463 is potent in ALK-driven preclinical models and in a variety of crizotinib-resistant models. AZD3463 inhibits ALK in cells as demonstrated by its ability to decrease ALK autophosphorylation in tumor cell lines containing ALK fusions including DEL (ALCL NPM-ALK), H3122 (NSCLC EML4-ALK) and H2228 (NSCLC EML4-ALK). Inhibition of ALK is associated with perturbations in downstream signaling including ERK, AKT and STAT3 pathways leading to preferential inhibition of proliferation in the ALK fusion containing cell lines in vitro. AZD3463 retains good activity against a number of clinically relevant crizotinib resistant mutations including the gatekeeper mutant L1196M where equivalent potency to wild type ALK is observed in vitro and in vivo in EML4-ALK containing BAF3 cell lines. To further assess the potential ability of AZD3463 to overcome additional resistance mechanisms, antiproliferative activity is assessed in multiple crizotinib resistant cell lines independently derived in vitro from H3122 cells as well as a patient derived crizotinib relapsed model. These resistant cell lines contain multiple resistance mechanisms including the L1196M gatekeeper and T115Ins mutations, ALK amplification and/or secondary drivers including EGFR and IGF1R. AZD3463 retains antiproliferative potency within 4 fold of parental H3122 cells for 10 out of 12 of these acquired resistance models in vitro. [1]
in vivo AZD3463 also demonstrates the ability to dose dependently inhibit pALK in xenograft tumors in vivo resulting in stasis (H3122) or regression (DEL, H2228). [1]

プロトコル(参考用のみ)

カスタマーフィードバック

, , PLoS One, 2015, 10(11):e0142704.

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：

Selective Impact of ALK and MELK Inhibition on ERα Stability and Cell Proliferation in Cell Lines Representing Distinct Molecular Phenotypes of Breast Cancer [ bioRxiv, 2023, 10.1101/2023.12.19.572304] PubMed: none
CD26 upregulates proliferation and invasion in keloid fibroblasts through an IGF-1-induced PI3K/AKT/mTOR pathway [ Burns Trauma, 2020, 8:tkaa025] PubMed: 33150188
A Human Organoid Model of Aggressive Hepatoblastoma for Disease Modeling and Drug Testing [ Cancers (Basel), 2020, 12(9)E2668] PubMed: 32962010
Identification of SYK Inhibitor, R406 as a Novel Senolytic Agent [ Aging (Albany NY), 2020, 7;12(9):8221-8240] PubMed: 32379705
Glycogen synthase kinase 3 controls migration of the neural crest lineage in mouse andXenopus [ Nature Communications, 2018, 1126-2018)] PubMed: None
Glycogen synthase kinase 3 controls migration of the neural crest lineage in mouse and Xenopus. [ Nat Commun, 2018, 9(1):1126] PubMed: 29555900
Vorinostat Enhances Cytotoxicity of SN-38 and Temozolomide in Ewing Sarcoma Cells and Activates STAT3/AKT/MAPK Pathways [Sampson VB, et al. PLoS One, 2015, 10(11):e0142704] PubMed: 26571493

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。