AZD1208

製品コードS7104 バッチS710404

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	C₂₁H₂₁N₃O₂S
	分子量	379.48	CAS No.	1204144-28-4
Solubility (25°C)*	体外	DMSO	75 mg/mL warmed with 50ºC water bath (197.63 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	AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
in vitro	AZD1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of Pim-1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. This is accompanied by a dose-dependent reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition, AZD1208 leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. ^[1]
in vivo	AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. ^[1]
特徴	Orally bioavailable Pim kinase inhibitor that has been tested in Phase I clinical trials for treatment of advanced solid tumors and malignant lymphoma.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDSCs
	濃度	1 μM
	反応時間	4 h
	実験の流れ	Bone marrow derived MDSCs were separated into M-MDCSs and suppressive neutrophils by FACS, then plated in RPMI with 10% FBS in the presence of DMSO or AZD1208 for 4 hours on coverslips.
動物実験	動物モデル	Female CB17 SCID mice
	投薬量	10 & 30 mg/kg
	投与方法	o.g.

参考

カスタマーフィードバック

: , , Blood, 2016, 127(20):2439-50.

: Data from [Data independently produced by , , Leukemia, 2018, 32(3):597-605]

: Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(4):849-857]

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：

2-Desaza-annomontine (C81) impedes angiogenesis through reduced VEGFR2 expression derived from inhibition of CDC2-like kinases [ Angiogenesis, 2024, 10.1007/s10456-024-09906-y]	PubMed: 38403816
CDK9 inhibition induces epigenetic reprogramming revealing strategies to circumvent resistance in lymphoma [ Mol Cancer, 2023, 22(1):64]	PubMed: 36998071
Nuclear transport surveillance of p53 by nuclear pores in glioblastoma [ Cell Rep, 2023, S2211-1247(23)00893-8]	PubMed: 37552992
Targeting macrophagic PIM-1 alleviates osteoarthritis by inhibiting NLRP3 inflammasome activation via suppressing mitochondrial ROS/Cl- efflux signaling pathway [ J Transl Med, 2023, 21(1):452]	PubMed: 37422640
Pivotal role of PIM2 kinase in plasmablast generation and plasma cell survival, opening new treatment options in myeloma [ Blood, 2022, blood.2021014011]	PubMed: 35108359
Targeting PIM2 by JP11646 results in significant antitumor effects in solid tumors [ Int J Oncol, 2022, 61(4)114]	PubMed: 35920189
Suppressive neutrophils require PIM1 for metabolic fitness and survival during chronic viral infection [ Cell Rep, 2021, 35(8):109160]	PubMed: 34038722
Feedback Loop Regulation Between Pim Kinases and Tax Keeps HTLV-I Viral Replication in Check [ J Virol, 2021, JVI0196021]	PubMed: 34818069
Co-Targeting PIM Kinase and PI3K/mTOR in NSCLC [ Cancers (Basel), 2021, 13(9)2139]	PubMed: 33946744
C81-evoked inhibition of the TNFR1-NFκB pathway during inflammatory processes for stabilization of the impaired vascular endothelial barrier for leukocytes [ FASEB J, 2021, 35(6):e21656]	PubMed: 34042211

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。