Tucatinib

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

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