AT13148

製品コードS7563 バッチS756301

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

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
* <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 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
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, AT13148 also inhibits AKT and p70S6K signaling. [1]
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. [1]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro kinase assays
AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 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 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.

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.]

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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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