Tucatinib

Catalog No.S8362 Synonyms: Irbinitinib, ONT-380, ARRY-380

For research use only.

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.

Tucatinib  Chemical Structure

CAS No. 937263-43-9

Selleck's Tucatinib has been cited by 9 Publications

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Biological Activity

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.
Targets
p95 HER2 [2]
(Cell-based assay)
ErbB2 [2]
(Cell-based assay)
7 nM 8 nM
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].

Assay
Methods Test Index PMID
Western blot p-HER2 / HER2 / p-AKT / AKT / p-ERK / ERK 30370249
Growth inhibition assay Cell viability 30670633
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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 480.52
Formula

C26H24N8O2

CAS No. 937263-43-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05230810 Not yet recruiting Drug: Alpelisib|Drug: Tucatinib|Drug: Fulvestrant HER2-positive Metastatic Breast Cancer Criterium Inc.|Novartis|Seagen Inc. August 1 2022 Phase 1|Phase 2
NCT05458674 Not yet recruiting Drug: Tucatinib|Drug: Eribulin|Drug: Trastuzumab Breast Cancer Criterium Inc. August 1 2022 Phase 2
NCT05382364 Recruiting Drug: Tucatinib Metastatic HER2+ Advanced Breast Cancer|Breast Neoplasms|Gastric or Gastroesophageal Junction Adenocarcinoma (GEC)|Colorectal Cancer Merck Sharp & Dohme LLC June 29 2022 Phase 1
NCT04512261 Withdrawn Drug: Tucatinib|Drug: Pembrolizumab|Drug: Trastuzumab Breast Cancer|Brain Metastases|HER2-positive Breast Cancer|CNS Disease Reva Basho|Merck Sharp & Dohme LLC|Seagen Inc.|Cedars-Sinai Medical Center June 1 2022 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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