1184263-99-7
1184263-99-7
Chemical Structure
Lapatinib-d4
Synonym(s): GW572016-d4;GW2016-d4
- CAS No.: 1184263-99-7
- Formula:C29H22D4ClFN4O4S
- Molecular Weight:585.08
IUPAC Name: 6-chloro-4H-benzo[e][1,2,4]thiadiazine-7-sulfonamide-3-13C-2-15N-15N 1,1-dioxide
InChIKey: BCFGMOOMADDAQU-AREBVXNXSA-N
SMILES: CS(C([2H])([2H])C([2H])([2H])NCC1=CC=C(O1)C2=CC(C(NC3=CC(Cl)=C(C=C3)OCC4=CC(F)=CC=C4)=NC=N5)=C5C=C2)(=O)=O
Biological Activity: Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib 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 | 99.02% | Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib 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 (Standard) | 99.69% | Lapatinib (Standard) is the analytical standard of Lapatinib. This product is intended for research and analytical applications. Lapatinib (GW572016) 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-d4-1 | Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) 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-d5 | Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) 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-d7 dihydrochloride | Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride 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-13C,d7 | Lapatinib-13C,d7 (GW572016-13C,d7) is the deuterium and 13C-labeled Lapatinib (HY-50898). Lapatinib (GW572016) 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-d7 | Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) 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 | 99.83% | Lapatinib (GW572016) 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]
