2749856-05-9
2749856-05-9
Chemical Structure
Lapatinib-d4 tosylate
Synonym(s): GW572016-d4 tosylate; GW2016-d4 tosylate
- CAS No.: 2749856-05-9
- Formula:C36H30D4ClFN4O7S2
- Molecular Weight:757.28
SMILES: O=S(O)(C1=CC=C(C=C1)C)=O.CS(C([2H])([2H])C([2H])([2H])NCC2=CC=C(O2)C3=CC(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N6)=C6C=C3)(=O)=O
Biological Activity: Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].
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Lapatinib-d4 tosylate | Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively. | |||||||||||||||||||||
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Lapatinib tosylate | Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively. | |||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. Rusnak DW, et al. 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):85-94 [Content Brief]
