BI-847325

製品コードS7843 バッチS784301

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

C₂₉H₂₈N₄O₂

分子量

464.56

CAS No.

1207293-36-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

19 mg/mL (40.89 mM)

Ethanol

1 mg/mL (2.15 mM)

Water

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.

* <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. This compound 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 this compound 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

https://pubmed.ncbi.nlm.nih.gov/25873592/

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。

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。