Vistusertib (AZD2014)

製品コードS2783 バッチS278302

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	92 mg/mL (198.9 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	Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
in vitro	AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. ^[1]
in vivo	AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates. ^[1]

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

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：

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
Culture and multiomic analysis of lung cancer patient-derived pleural effusions revealed distinct druggable molecular types [ Sci Rep, 2022, 12(1):6345]	PubMed: 35428753
[The dual mTORC1/2 inhibitor AZD2014 inhibits acute graft rejection in a rat liver transplantation model] [ Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(4):598-603]	PubMed: 35527497
SARS-CoV-2 infection rewires host cell metabolism and is potentially susceptible to mTORC1 inhibition [ Nat Commun, 2021, 12(1):1876]	PubMed: 33767183
Multifocal Organoid Capturing of Colon Cancer Reveals Pervasive Intratumoral Heterogenous Drug Responses [ Adv Sci (Weinh), 2021, e2103360]	PubMed: 34918496

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。