Fisogatinib (BLU-554)

製品コードS8503 バッチS850302

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

C₂₄H₂₄Cl₂N₄O₄

分子量

503.38

CAS No.

1707289-21-1

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (198.65 mM)

Ethanol (warmed with 50ºC water bath)

2 mg/mL (3.97 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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (9.93mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (0.99mM)

* <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	Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.
in vitro	Fisogatinib (BLU-554) exploits a unique interaction with FGFR4 to confer potency and selectivity
in vivo	Fisogatinib (BLU-554) is well tolerated in these tumor models, and administration of this compound induces tumor regression in liver cancer models^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	ST8814 resistant cells
	濃度	1 µM
	反応時間	4 h
	実験の流れ	ST8814 resistant cells were treated with DMSO or Fisogatinib (BLU-554) at 1 µM for 4 hrs.
動物実験	動物モデル	Male FVB/NRj mice
	投薬量	10 mg/kg
	投与方法	p.o.

参考

http://media.ilc-congress.eu/wp-content/uploads/2015/04/Dr-Klaus-Hoeflich_Friday-Press-Conference.pdf
https://pubmed.ncbi.nlm.nih.gov/33203698/
https://pubmed.ncbi.nlm.nih.gov/30802754/

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：

Molecular Interaction of Soluble Klotho with FGF23 in the Pathobiology of Aortic Valve Lesions Induced by Chronic Kidney Disease [ Int J Biol Sci, 2024, 20(9):3412-3425]	PubMed: 38993571
Fibroblast Growth Factor Receptor 4 Promotes Triple-Negative Breast Cancer Progression via Regulating Fatty Acid Metabolism Through the AKT/RYR2 Signaling [ Cancer Med, 2024, 13(23):e70439]	PubMed: 39658878
FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(24):e2302613]	PubMed: 37345586
Carcinoma of the human adrenal cortex: identification and in vitro and in vivo study of molecular alterations as potential therapeutic targets [ UNIVERSITY OF BRESCIA, 2023, ]	PubMed: None
Fibroblast growth factor receptor 4 promotes glioblastoma progression: a central role of integrin-mediated cell invasiveness [ Acta Neuropathol Commun, 2022, 10(1):65]	PubMed: 35484633
BLU-554, A selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro [ Biochem Biophys Res Commun, 2022, 595:22-27]	PubMed: 35093636
EGFR activation limits the response of liver cancer to lenvatinib [ Nature, 2021, 595(7869):730-734]	PubMed: 34290403
Activation of receptor tyrosine kinases mediates acquired resistance to MEK inhibition in malignant peripheral nerve sheath tumors [ Cancer Res, 2020, canres.1992.2020]	PubMed: 33203698
Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy [ Cancers (Basel), 2020, 12(8):E2010]	PubMed: 32708005
Protein tyrosine kinase 2: a novel therapeutic target to overcome acquired EGFR-TKI resistance in non-small cell lung cancer [ Respir Res, 2019, 20(1-:270]	PubMed: 31791326

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。