Tucatinib

Name: Tucatinib
Brand: Tocris Bioscience
SKU: 7640

Tocris Bioscience, part of Bio-Techne | Catalog # 7640

COA / SDS

Potent and selective ErbB2 inhibitor

Key Product Details

Description:	Potent and selective ErbB2 inhibitor
Chemical Name:	N⁶-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N⁴-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine
Purity:	≥98% (HPLC)
Molecular Weight:	480.52

View Full Technical Details for Tucatinib

Technical Data
Citations

Biological Activity for Tucatinib

Tucatinib is a potent and selective ErbB-2 (also called HER2) kinase inhibitor (IC₅₀ = 7 nM). It exhibits >50-fold selectivity for ErbB-2 over EGFR. In vitro, Tucatinib inhibits ErbB-2 signaling activity and cell proliferation in ErbB-2-amplified breast cancer cell lines (BT-474). In vivo, Tucatinib (25-100 mg/kg) reduces tumor volume in breast and gastric xenograft mouse models.This compound is orally bioavailable.

Compound Libraries for Tucatinib

Tucatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Tucatinib

M. Wt	480.52
Formula	C₂₆H₂₄N₈O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	937263-43-9
PubChem ID	51039094
InChi Key	SDEAXTCZPQIFQM-UHFFFAOYSA-N
Smiles	N=1C=NC(NC2=CC=C(OC=3C=CN4N=CN=C4C3)C(=C2)C)=C5C=C(C=CC15)NC6=NC(C)(C)CO6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Tucatinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	48.05	100

Preparing Stock Solutions for Tucatinib

The following data is based on the product molecular weight 480.52.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.08 mL	10.41 mL	20.81 mL
5 mM	0.42 mL	2.08 mL	4.16 mL
10 mM	0.21 mL	1.04 mL	2.08 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for Tucatinib

References are publications that support the biological activity of the product.

Kulukian Preclinical activity of HER2-selective Tyrosine Kinase inhibitor Tucatinib as a single agent or in combination with Trastuzumab or Docetaxel in solid tumor models. Mol.Cancer.Ther. 2020 PMID: 32241871