LY3295668

製品コードS8782 バッチS878201

印刷

化学情報

Synonyms

AK-01

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₄H₂₆ClF₂N₅O₂

分子量

489.95

CAS No.

1919888-06-4

Solubility (25°C)*

体外

DMSO

98 mg/mL (200.02 mM)

Ethanol

15 mg/mL (30.61 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	LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
in vitro	LY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1^mut cancer cells.^[1]
in vivo	LY3295668 leads to durable regression of RB1^mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for this compound cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NCI-H446 cells, Calu-6 cells
	濃度	0.001 μM - 1 μM
	反応時間	24 h, 48 h, 72 h
	実験の流れ	To measure apoptosis by IncuCyte Zoom instrument, NCI-H446 and Calu-6 cells are plated on Costar 3596 plates and treated with LY3295668 at different concentrations for 24, 48, and 72 hours. Caspase 3/7 activation is measured with Cell- Player 96-Well Kinetic Caspase 3/7 reagent. Green fluorescent images are acquired every 2 hours. Green objects counted (y-axis) are plotted against either real time (x-axis) or raw numbers as percent control.
動物実験	動物モデル	7–8 week-old athymic nude female mice
	投薬量	50 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/30373917/

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：

AURKA Suppresses Ferroptosis via the KEAP1/NRF2/HO‑1 Axis in EGFR-Mutant Lung Adenocarcinoma [ Front Biosci (Landmark Ed), 2025, 30(8):41293]	PubMed: 40917063
RET overexpression leads to increased brain metastatic competency in luminal breast cancer [ J Natl Cancer Inst, 2024, djae091]	PubMed: 38852945
Combination of an aurora kinase inhibitor and the ABL tyrosine kinase inhibitor asciminib against ABL inhibitor-resistant CML cells [ Med Oncol, 2024, 41(6):142]	PubMed: 38714583
Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752]	PubMed: 37572644
Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752]	PubMed: 37572644
BCL-xL inhibition potentiates cancer therapies by redirecting the outcome of p53 activation from senescence to apoptosis [ Cell Rep, 2022, 41(12):111826]	PubMed: 36543138
Treatment of RB-deficient retinoblastoma with Aurora-A kinase inhibitor [ Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469]	PubMed: 34741392

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。