BI-847325

製品コードS7843 バッチS784301

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	C₂₉H₂₈N₄O₂
	分子量	464.56	CAS No.	1207293-36-4
Solubility (25°C)*	体外	DMSO	19 mg/mL warmed with 50ºC water bath (40.89 mM)
		Ethanol	1 mg/mL (2.15 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	BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
in vitro	BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. ^[1]
in vivo	In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells
	濃度	30 μM
	反応時間	72 h
	実験の流れ	Cells are plated at a density of 2.5 × 10³ cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturer's protocol.
動物実験	動物モデル	Mice bearing 1205Lu and 1205LuR xenografts
	投薬量	70 mg/kg
	投与方法	p.o.

参考

[1] Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364.

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：

Salmonella effector SopB reorganizes cytoskeletal vimentin to maintain replication vacuoles for efficient infection [ Nat Commun, 2023, 14(1):478]	PubMed: 36717589
High In Vitro and In Vivo Activity of BI-847325, a Dual MEK/Aurora Kinase Inhibitor, in Human Solid and Hematologic Cancer Models [ Cancer Res Commun, 2023, 3(10):2170-2181]	PubMed: 37830744
High In Vitro and In Vivo Activity of BI-847325, a Dual MEK/Aurora Kinase Inhibitor, in Human Solid and Hematologic Cancer Models [ Cancer Res Commun, 2023, 3(10):2170-2181]	PubMed: 37830744
GANT61/BI-847325 combination: a new hope in lung cancer treatment [ Med Oncol, 2022, 39(10):144]	PubMed: 35834029
A survey of the kinome pharmacopeia reveals multiple scaffolds and targets for the development of novel anthelmintics [ Sci Rep, 2021, 11(1):9161]	PubMed: 33911106
CAGE-prox: A Unified Approach for Time-Resolved Protein Activation in Living Systems [ Curr Protoc, 2021, 1(6):e180]	PubMed: 34165886
Time-resolved protein activation by proximal decaging in living systems [Wang J, et al. Nature, 2019, 569(7757):509-513]	PubMed: 31068699
The Novel ATP-Competitive MEK/Aurora Kinase Inhibitor BI-847325 Overcomes Acquired BRAF Inhibitor Resistance through Suppression of Mcl-1 and MEK Expression. [ Mol Cancer Ther, 2015, 14(6):1354-64]	PubMed: 25873592

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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