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Lapatinib ditosylate
- GW 572016
- Parent CAS: 231277-92-2
- Soluble in DMSO
- MF: C29H26ClFN4O4S.2C7H8O3S
- MW: 925.46
Description
Lapatinib ditosylate is a reversible, ATP-competitive dual EGFR/HER2 tyrosine kinase inhibitor that inhibits signaling by ERBB1 and ERBB2.
Lapatinib blocks receptor phosphorylation and downstream MAPK and PI3K–AKT pathways in HER2- or EGFR-dependent cells. It is a standard pharmacological tool for HER-family signaling, receptor crosstalk and resistance mechanisms.
Key Features
- Dual EGFR and HER2 kinase inhibitor
- ATP-competitive and reversible mechanism
- Suppresses HER-family downstream signaling
- Clinically established HER2-targeted pharmacology
Applications
- EGFR and HER2 kinase assays
- HER2-positive cancer models
- ERBB receptor crosstalk studies
- Resistance and combination-treatment research
More Information
| Parent CAS No. | 231277-92-2 |
|---|---|
| Chemical Name | N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl] quinazolin-4-amine ditosylate |
| SMILES | O1C(C2C=CC3=NC=NC(NC4C=C(Cl)C(OCC5C=CC=C(F)C=5)=CC=4)=C3C=2)=CC=C1CNCCS(C)(=O)=O.C1C=C(C)C=CC=1S(O)(=O)=O.C1C=C(C)C=CC=1S(O)(=O)=O |
| MFCD | MFCD09264195 |
| InChi | InChI=1S/C29H26ClFN4O4S.2C7H8O3S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19;2*1-6-2-4-7(5-3-6)11(8,9)10/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*2-5H,1H3,(H,8,9,10) |
| InChiKey | UWYXLGUQQFPJRI-UHFFFAOYSA-N |
| CID | 9941095 |
| Short Description | EGFR/ErbB-2 inhibitor |
References
- HA Burris. Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist 2004, 9 Suppl 3: 10–5.
- MH Nelson, CR Dolder. Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother 2006, 40(2), 261–9.
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