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Formula | C26H24N8O2 |
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Molecular Weight | 480.52 | CAS No. | 937263-43-9 | |
Solubility (25°C)* | In vitro | DMSO | 96 mg/mL (199.78 mM) | |
Ethanol | 15 mg/mL (31.21 mM) | |||
Water | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity. | ||||
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Targets |
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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]. |
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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]. |
Cell Assay: |
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Animal Study: |
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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 |
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 |
Využití vybraných inhibitorů k překonání anthracyklinové rezistence v terapii nádorových onemocnění (in vitro studie). [ Charles University, 2023, ] | PubMed: None |
Metabolic diversity within breast cancer brain-tropic cells determines metastatic fitness [ Cell Metab, 2022, 34(1):90-105.e7] | PubMed: 34986341 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.