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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
Biological Activity
Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
Targets
Target | Value |
---|---|
ErbB2 | IC50: 9.2nM |
EGFR | IC50: 10.8nM |
ErbB4 | IC50: 367nM |
c-Src | IC50: 3.5μM |
C-Raf-1 | IC50: >10μM |
MEK | IC50: >10μM |
ERK | IC50: >10μM |
c-Fms | IC50: >10μM |
CDK1 | IC50: >10μM |
CDK2 | IC50: >10μM |
p38 | IC50: >10μM |
Tie-2 | IC50: >10μM |
VEGFR2 | IC50: >10μM |
In vitro (25°C) | DMSO | 99 mg/mL (170.37 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 9 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 17.21 mL | 86.04 mL | 172.09 mL |
0.5 mM | 3.44 mL | 17.21 mL | 34.42 mL |
1 mM | 1.72 mL | 8.6 mL | 17.21 mL |
5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
*The above data is based on the productmolecular weight 581.1 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A11752 |
---|---|
CAS No. | 231277-92-2 |
Formula | C29H26ClFN4O4S |
M. Wt | 581.1 |
Purity | >98% |
SMILES | CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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