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Tucatinib (Irbinitinib, ONT-380, Arry-380) HER2 inhibitor

Name: Tucatinib (Irbinitinib, ONT-380, Arry-380)
Brand: Selleck Chemicals
SKU: S8362
Availability: InStock
Rating: 5 (28 reviews)

Cat.No.S8362

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.

Chemical Structure

Molecular Weight: 480.52

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	EGFR VEGFR FGFR PDGFR c-Met Src MEK CSF-1R FLT3 c-Kit
Other HER2 Inhibitors	Sevabertinib (BAY 2927088) CP-724714 Sapitinib (AZD8931) Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 Zongertinib (BI 1810631) TAS0728 IAM1363

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.
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.
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	480.52	Formula	C₂₆H₂₄N₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	937263-43-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Irbinitinib, ONT-380, ARRY-380			SMILES	CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	p95 HER2 (Cell-based assay) 7 nM ErbB2 (Cell-based assay) 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. In cell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2.
In vivo	In vivo, ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models. 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).
References	[1] http://cancerres.aacrjournals.org/content/69/24_Supplement/5104 [2] http://assets.cureus.com/uploads/poster/file/91/e.pdf [3] https://pubmed.ncbi.nlm.nih.gov/30370249/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-HER2 / HER2 / p-AKT / AKT / p-ERK / ERK		30370249
Growth inhibition assay	Cell viability		30670633

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-28)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07768358	NOT_YET_RECRUITING	HER2-positive Breast Cancer; Cervical Cancer; Biliary Tract Neoplasms; Urothelial Cancer; Advanced Non-Small Cell Lung Cancer; Gastric or Gastroesophageal Junction Adenocarcinoma (GEC); Colorectal Cancer	Pfizer	2026-11-06	PHASE4
NCT05868226	RECRUITING	HER2-positive Breast Cancer; Metastatic Cancer; Metastatic Breast Cancer; Metastatic; HER2-positive Metastatic Breast Cancer; HER2 Mutation-Related Tumors; HER-2 Protein Overexpression; HER2-negative Breast Cancer; Triple Negative Breast Cancer; HR Positive; Hormone Receptor-positive Breast Cancer; Estrogen Receptor Positive Tumor; Progesterone Receptor-positive Breast Cancer; Hormone Receptor Negative Breast Carcinoma; Solid Tumor; Solid Tumor, Adult; Solid Carcinoma; HER2 Low Breast Cancer; HER2 Low Breast Carcinoma; ER Positive Breast Cancer; PR-positive Breast Cancer; Minimal Residual Disease; Colo-rectal Cancer; Colon Cancer; Rectal Cancer; ctDNA Monitoring; Colorectal Neoplasms; Colonic Neoplasms; Rectal Neoplasms; Neoplasm, Residual; Adenocarcinoma of Colon; Adenocarcinoma	QuantumLeap Healthcare Collaborative	2023-02-15	PHASE1; PHASE2
NCT01042379	RECRUITING	Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer	QuantumLeap Healthcare Collaborative	2010-03-01	PHASE2
NCT06686394	RECRUITING	Breast Neoplasms; Breast Cancer	Merck Sharp & Dohme LLC	2025-02-26	PHASE1; PHASE2
NCT06439693	RECRUITING	Breast Cancer Female; Breast Cancer; Breast Cancer Metastatic; Estrogen Receptor-positive Breast Cancer; HER2-positive Breast Cancer; Stage IV Breast Cancer	Dana-Farber Cancer Institute	2024-08-08	PHASE2
NCT06157892	ACTIVE_NOT_RECRUITING	Breast Neoplasms; Gastroesophageal Junction Adenocarcinoma; HER2 Low Breast Neoplasms; HER2 Positive Breast Neoplasms; Stomach Neoplasms; Triple Negative Breast Neoplasms; Metastatic Breast Cancer; Metastatic Gastric Cancer; Advanced Breast Cancer; Advanced Gastric Cancer	Seagen, a wholly owned subsidiary of Pfizer	2024-05-20	PHASE2

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