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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 (24 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 PDGFR FGFR c-Met Src MEK CSF-1R FLT3 c-Kit
Other HER2 Inhibitors	CP-724714 Sapitinib (AZD8931) Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 Zongertinib TAS0728

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

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 2024-05-22)

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

Tech Support

Handling Instructions

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