AZD0364 (ATG-017)

製品コードS8708 バッチS870801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₄H₂₄F₂N₈O₂
	分子量	494.50	CAS No.	2097416-76-5
Solubility (25°C)*	体外	DMSO	99 mg/mL (200.2 mM)
		Ethanol	99 mg/mL (200.2 mM)
		Water	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	AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
in vitro	AZD0364 exhibits high cellular potency against a direct downstream substrate on the MAPK pathway (e.g. inhibition of phospho-p90RSK1 in BRAFV600E mutant A375 cells, IC50 = 6 nM). The molecule is a highly selective kinase inhibitor (10/329 kinases tested are inhibited at >50% at a 1 µM) and has long residence time on the protein (as determined by SPR on human unphosphorylated-ERK2: pKd = 10; t1/2 = 277 mins)^[2].
in vivo	AZD0364 has good oral pharmacokinetics across species. In xenograft models, AZD0364 inhibits phospho-p90RSK1 in tumors in a dose-dependent manner. AZD0364 induces regressions in the KRAS mutant NSCLC Calu 6 xenograft model. AZD0364 can also be combined safely and effectively with the MEK1/2 inhibitor selumetinib in KRAS mutant NSCLC xenograft models^[2].

プロトコル(参考用のみ)

参考

[1] Richard Andrew Ward, et al. Dihydroimidazopyrazinone derivatives useful in the treatment of cancer. WO2017080979A1.
[2] Iain Simpson, et al. AACR Cancer Res. 2018, 78(13 Suppl):Abstract nr 1647.

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：

Investigating the Role of TGF-β Signaling Pathways in Human Corneal Endothelial Cell Primary Culture [ Cells, 2023, 12(12)1624]	PubMed: 37371094
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2 [ bioRxiv, 2023, 2023.09.12.557258]	PubMed: 37745518
Non-canonical Targets of HIF1a Impair Oligodendrocyte Progenitor Cell Function [ Cell Stem Cell, 2021, 28(2):257-272.e11]	PubMed: 33091368
Targeting the MAPK/ERK and PI3K/AKT Signaling Pathways Affects NRF2, Trx and GSH Antioxidant Systems in Leukemia Cells [ Antioxidants (Basel), 2020, 9(7)E633]	PubMed: 32709140
Targeting the MAPK/ERK and PI3K/AKT Signaling Pathways Affects NRF2, Trx and GSH Antioxidant Systems in Leukemia Cells [ Antioxidants (Basel), 2020, 9(7):633]	PubMed: 32709140

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。