Pricing Availability   Qty
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)
Literature (1)

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
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 Data for Tucatinib

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for Tucatinib

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

Kulukian et al (2020) 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. 19 976 PMID: 32241871

If you know of a relevant reference for Tucatinib, please let us know.

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Citations for Tucatinib

Citations are publications that use Tocris products.

Currently there are no citations for Tucatinib. Do you know of a great paper that uses Tucatinib from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.