Vistusertib (AZD2014)

製品コードS2783 バッチS278304

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

C₂₅H₃₀N₆O₃

分子量

462.54

CAS No.

1009298-59-2

Solubility (25°C)*

体外

DMSO

46 mg/mL (99.45 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 30%PEG300 2 65%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。	5.000mg/ml (10.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. 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	Vistusertib (AZD2014)は、cell-freeアッセイにおいて2.8 nMのIC50値を示す新規mTOR阻害剤であり、複数のPI3Kアイソフォーム（α/β/γ/δ）に対して高い選択性を示します。AZD2014を1 μMで試験した場合、ほとんどのキナーゼに対して結合が認められないか、弱い結合でした。AZD2014は、抗腫瘍活性を有するHCC細胞において、増殖抑制、apoptosis、細胞周期停止、およびautophagyを誘導します。
in vitro	Vistusertib (AZD2014) is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. It has greater inhibitory activity against mTORC1 compared to rapamycin: this compound decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. It also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, it induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy.
in vivo	Vistusertib (AZD2014) induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	2.81 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Male SCID mice
	投薬量	20 mg/kg
	投与方法	p.o.

参考

http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/917?rss=1
https://pubmed.ncbi.nlm.nih.gov/26358751/

カスタマーフィードバック

: Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

: Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

: Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

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：

Elevated NR2F1 underlies the persistence of invasive disease after treatment of BRAF-mutant melanoma [ J Clin Invest, 2025, 135(18)e178446]	PubMed: 40955663
A phase II trial of mTORC1/2 inhibition in STK11 deficient non small cell lung cancer [ NPJ Precis Oncol, 2025, 9(1):67]	PubMed: 40069402
Volatilomic response to targeted cancer therapy in vitro [ Sci Rep, 2025, 15(1):19445]	PubMed: 40461777
Effects of simulated microgravity on colorectal cancer organoids growth and drug response [ Sci Rep, 2024, 14(1):25526]	PubMed: 39462078
USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities [ Cell Rep Med, 2023, 4(4):101007]	PubMed: 37030295
m7G-related genes predict prognosis and affect the immune microenvironment and drug sensitivity in osteosarcoma [ Front Pharmacol, 2023, 14:1158775]	PubMed: 37654606
Co-Targeting FASN and mTOR Suppresses Uveal Melanoma Growth [ Cancers (Basel), 2023, 15(13)3451]	PubMed: 37444561
Drug-Dependent Morphological Transitions in Spherical and Worm-Like Polymeric Micelles Define Stability and Pharmacological Performance of Micellar Drugs [ Small, 2022, 18(4):e2103552]	PubMed: 34841670
High-risk neuroblastoma with NF1 loss of function is targetable using SHP2 inhibition [ Cell Rep, 2022, 40(4):111095]	PubMed: 35905710
Reciprocal effects of mTOR inhibitors on pro-survival proteins dictate therapeutic responses in tuberous sclerosis complex [ iScience, 2022, 25(11):105458]	PubMed: 36388985

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。