Home Protein Tyrosine Kinase HER2 inhibitor - EGFR inhibitor Tucatinib For research use only.

Tucatinib

Synonyms: Irbinitinib, ONT-380, ARRY-380

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

Tucatinib Chemical Structure

CAS No. 937263-43-9

Purity & Quality Control

Tucatinib Related Products

Signaling Pathway

HER2 Signaling Pathways

HER2 Signaling Pathway

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
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].
Cell Research Cell lines ZR75.1, SKBR3, BT474 and NZBR3 cells
Concentrations 380 μM
Incubation Time 24 h
Method

Cells were treated with ARRY-380 for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-HER2 / HER2 / p-AKT / AKT / p-ERK / ERK 30370249
Growth inhibition assay Cell viability 30670633
In Vivo
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].
Animal Research Animal Models Nude mice
Dosages ranging up to 200 mg/kg/d
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05458674 Recruiting
Breast Cancer
Criterium Inc.
 January 1 2024 Phase 2
NCT05748834 Recruiting
Breast Cancer
SCRI Development Innovations LLC|Seagen Inc.
 July 24 2023 Phase 2
NCT05892068 Recruiting
Metastatic Breast Cancer
Memorial Sloan Kettering Cancer Center|Seagen Inc.
 May 9 2023 Phase 2
NCT05230810 Recruiting
HER2-positive Metastatic Breast Cancer
Criterium Inc.|Novartis|Seagen Inc.
 August 25 2022 Phase 1|Phase 2
NCT05382364 Active not recruiting
Metastatic HER2+ Advanced Breast Cancer|Breast Neoplasms|Gastric or Gastroesophageal Junction Adenocarcinoma (GEC)|Colorectal Cancer
Merck Sharp & Dohme LLC
 June 29 2022 Phase 1

Chemical Information & Solubility

Molecular Weight 480.52 Formula

C26H24N8O2
CAS No. 937263-43-9 SDF Download Tucatinib SDF
Smiles CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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