Roblitinib (FGF401)

製品コードS8548 バッチS854802

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

C₂₅H₃₀N₈O₄

分子量

506.56

CAS No.

1708971-55-4

Solubility (25°C)*

体外

DMSO

6 mg/mL (11.84 mM)

Water

Insoluble

Ethanol

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。	0.500mg/ml (0.99mM)
	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	Roblitinib (FGF401)は、IC50が1.9 nMのFGFR4選択的阻害剤です。これは可逆的共有結合様式でFGFR4キナーゼドメインに結合し、生化学アッセイで65キナーゼのパネルに対して少なくとも1,000倍の選択性を示します。
in vitro	Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and inhibits it with an IC50 of 1.9 nM. In biochemical assays, this compound shows at least 1,000 fold selectivity against a panel of 65 kinases, and in a kinome wide scan consisting of 456 kinases, FGFR4 was its only target. It also inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho.
in vivo	In xenograft animal models in vivo, Roblitinib (FGF401) showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB.

製品説明

Roblitinib (FGF401)は、IC50が1.9 nMのFGFR4選択的阻害剤です。これは可逆的共有結合様式でFGFR4キナーゼドメインに結合し、生化学アッセイで65キナーゼのパネルに対して少なくとも1,000倍の選択性を示します。

in vitro

Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and inhibits it with an IC50 of 1.9 nM. In biochemical assays, this compound shows at least 1,000 fold selectivity against a panel of 65 kinases, and in a kinome wide scan consisting of 456 kinases, FGFR4 was its only target.

It also inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho.

in vivo

In xenograft animal models in vivo, Roblitinib (FGF401) showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	1.9 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Male Wistar Hannover rats
	投薬量	10, 30, 100 mg/kg
	投与方法	o.g.

参考

http://cancerres.aacrjournals.org/content/77/13_Supplement/2098
https://pubmed.ncbi.nlm.nih.gov/26615127/
http://cancerres.aacrjournals.org/content/77/13_Supplement/2103

https://patents.google.com/patent/WO2015059668A1

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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：

FGF receptor kinase inhibitors exhibit broad antiviral activity by targeting Src family kinases [ Cell Mol Life Sci, 2024, 81(1):471]	PubMed: 39621133
Multi-Omics Profiles of Small Intestine Organoids in Reaction to Breast Milk and Different Infant Formula Preparations [ Nutrients, 2024, 16(17)2951]	PubMed: 39275267
FGFR4 and EZH2 inhibitors synergistically induce hepatocellular carcinoma apoptosis via repressing YAP signaling [ J Exp Clin Cancer Res, 2023, 42(1):96]	PubMed: 37085881
Comprehensive multi-platform tyrosine kinase profiling reveals novel actionable FGFR aberrations across pediatric and AYA sarcomas [ bioRxiv, 2023, 10.1101/2023.07.19.548825]	PubMed: None
Strategies to inhibit FGFR4 V550L-driven rhabdomyosarcoma [ Br J Cancer, 2022, 10.1038/s41416-022-01973-6]	PubMed: 36097178
Comprehensive analysis of the prognostic value and immune infiltration of FGFR family members in gastric cancer [ Front Oncol, 2022, 12:936952]	PubMed: 36147913

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。