AT13148

製品コードS7563 バッチS756301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₁₆ClN₃O

分子量

313.78

CAS No.

1056901-62-2

Solubility (25°C)*

体外

DMSO

62 mg/mL (197.59 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.100mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 62 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.440mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	AT13148は、経口のATP競合的マルチAGCキナーゼ阻害剤で、Akt1/2/3、p70S6K、PKA、およびROCKI/IIに対するIC50値はそれぞれ38 nM/402 nM/50 nM、8 nM、3 nM、および6 nM/4 nMです。第1相。
in vitro	AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, this compound also inhibits AKT and p70S6K signaling.
in vivo	AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts.

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro kinase assays
キナーゼアッセイ	AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of this compound is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
細胞アッセイ	細胞株	MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines
	濃度	~10 μM
	反応時間	72 hours or 96 hours
	実験の流れ	Cytotoxicity of this compound is determined using a 72 h Alamar Blue assay or a 96 h SRB assay.
動物実験	動物モデル	Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
	投薬量	~50 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/22781553/

カスタマーフィードバック

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 478(1):330-6.]

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：

Therapeutic targeting of tumor spheroids in a 3D microphysiological renal cell carcinoma-on-a-chip system [ Neoplasia, 2023, 10.1016/j.neo.2023.100948]	PubMed: 37944353
Immunogenic Death of Hepatocellular Carcinoma Cells in Mice Expressing Caspase-Resistant ROCK1 Is Not Replicated by ROCK Inhibitors [ Cancers (Basel), 2022, 14(23)5943]	PubMed: 36497425
A preclinical pipeline to evaluate migrastatics as therapeutic agents in metastatic melanoma [ Br J Cancer, 2021, 10.1038/s41416-021-01442-6]	PubMed: 34172930
Discovery and Characterization of a Novel MASTL Inhibitor MKI-2 Targeting MASTL-PP2A in Breast Cancer Cells and Oocytes [ Pharmaceuticals (Basel), 2021, 14(7)647]	PubMed: 34358073
DAPL1 is a novel regulator of testosterone production in Leydig cells of mouse testis [ Sci Rep, 2021, 11(1):18532]	PubMed: 34535743
Study on the potential effect of multi-AGC kinase AT13148 on the Notch signaling pathway in glioblastoma [ Arch Med Sci, 2021, 10.5114/aoms/135083]	PubMed: None
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325
Myosin II Reactivation and Cytoskeletal Remodeling as a Hallmark and a Vulnerability in Melanoma Therapy Resistance. [ Cancer Cell, 2020, 37(1):85-103]	PubMed: 31935375
MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast Cancer [ Front Oncol, 2020, 10:571601]	PubMed: 33117702
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790]	PubMed: 31160710

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。