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Synonyms | Irbinitinib, ONT-380, ARRY-380 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H24N8O2 |
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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) |
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* <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. |
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. |
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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]. |
細胞アッセイ | 細胞株 | ZR75.1, SKBR3, BT474 and NZBR3 cells |
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濃度 | 380 μM | |
反応時間 | 24 h | |
実験の流れ | Cells were treated with ARRY-380 for 24 h. |
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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. |
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 |
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 |
High-throughput screen in vitro identifies dasatinib as a candidate for combinatorial treatment with HER2-targeting drugs in breast cancer [ PLoS One, 2023, 18(1):e0280507] | PubMed: 36706086 |
Metabolic diversity within breast cancer brain-tropic cells determines metastatic fitness [ Cell Metab, 2022, 34(1):90-105.e7] | PubMed: 34986341 |
Poziotinib Inhibits HER2-Mutant-Driven Therapeutic Resistance and Multiorgan Metastasis in Breast Cancer [ Cancer Res, 2022, 82(16):2928-2939] | PubMed: 35736563 |
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975] | PubMed: 36313330 |
miR-101-5p Acts as a Tumor Suppressor in HER2-Positive Breast Cancer Cells and Improves Targeted Therapy [ Breast Cancer (Dove Med Press), 2022, 14:25-39] | PubMed: 35256859 |
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。