Lapatinib-d4 (GW572016-d4) tosylate is a deuterated version of Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent and orally active inhibitor of ErbB-2 and EGFR tyrosine kinase domains with IC50 values of 10.2 and 9.8 nM for purified EGFR and ErbB-2, respectively.

Physicochemical Properties

Molecular Formula	C36H30D4CLFN4O7S2
Molecular Weight	757.28
CAS #	2749856-05-9
Related CAS #	Lapatinib tosylate;1187538-35-7
SMILES	ClC1=C(C=CC(=C1)NC1=C2C(C=CC(=C2)C2=CC=C(CNC([2H])([2H])C([2H])([2H])S(C)(=O)=O)O2)=NC=N1)OCC1C=CC=C(C=1)F.S(C1C=CC(C)=CC=1)(=O)(=O)O.S(C1C=CC(C)=CC=1)(=O)(=O)O
Synonyms	GW572016-d4 tosylate; GW2016-d4 tosylate
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94http://www.ncbi.nlm.nih.gov/pubmed/12467226.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.3205 mL	6.6026 mL	13.2052 mL
	5 mM	0.2641 mL	1.3205 mL	2.6410 mL
	10 mM	0.1321 mL	0.6603 mL	1.3205 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.