Tucatinib

製品コードS8362 バッチS836204

印刷

化学情報

Synonyms

Irbinitinib, ONT-380, ARRY-380

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₄N₈O₂

分子量

480.52

CAS No.

937263-43-9

Solubility (25°C)*

体外

DMSO

96 mg/mL (199.78 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.
Clear solution	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。	0.800mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 16 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
in vitro	The compound is a reversible, ATP-competitive inhibitor with nanomolar potency against ErbB2 in both in vitro and in cell-based assays^[1]. In cell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2^[2].
in vivo	In vivo, ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models^[2]. It shows excellent activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model, ARRY-380 demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size)^[1].

製品説明

Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.

in vitro

The compound is a reversible, ATP-competitive inhibitor with nanomolar potency against ErbB2 in both in vitro and in cell-based assays^[1].

In cell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2^[2].

in vivo

In vivo, ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models^[2].

It shows excellent activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model, ARRY-380 demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size)^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	ZR75.1, SKBR3, BT474 and NZBR3 cells
	濃度	380 μM
	反応時間	24 h
	実験の流れ	Cells were treated with ARRY-380 for 24 h.
動物実験	動物モデル	Nude mice
	投薬量	ranging up to 200 mg/kg/d
	投与方法	p.o.

参考

http://cancerres.aacrjournals.org/content/69/24_Supplement/5104
http://assets.cureus.com/uploads/poster/file/91/e.pdf
https://pubmed.ncbi.nlm.nih.gov/30370249/

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：

Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14]	PubMed: 40185092
Hotspot mutations in HER2 interfaces destabilize structure, causing breast cancer treatment failure [ Res Sq, 2025, rs.3.rs-5931887]	PubMed: 40166021
Peptidylarginine deiminase 3 modulates response to neratinib in HER2 positive breast cancer [ Oncogenesis, 2024, 13(1):30]	PubMed: 39097594
Neratinib plus dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo [ Transl Oncol, 2024, 49:102073]	PubMed: 39191139
HER4 and EGFR activate cell signaling in NRG1 fusion-driven cancers: implications for HER2/HER3-specific vs. pan-HER targeting strategies [ J Thorac Oncol, 2023, S1556-0864(23)00802-X]	PubMed: 37678511
Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532]	PubMed: 37596261
Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532]	PubMed: 37596261
Integrin αvβ3 Is a Master Regulator of Resistance to TKI-Induced Ferroptosis in HER2-Positive Breast Cancer [ Cancers (Basel), 2023, 15(4)1216]	PubMed: 36831558
Drug-drug interaction potentials of tucatinib inhibition of human UDP-glucuronosyltransferases [ Chem Biol Interact, 2023, 381:110574]	PubMed: 37263554
Novel HER2-targeted therapy to overcome trastuzumab resistance in HER2-amplified gastric cancer [ Sci Rep, 2023, 13(1):22648]	PubMed: 38114573

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。