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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Angiogenesis > LapatinibCAS：231277-92-2
Molecular Formula：C29H26ClFN4O4S
Molecular Weight：581.06
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 231277-92-2 |
| Name | Lapatinib |
| Molecular Formula | C29H26ClFN4O4S |
| Molecular Weight | 581.06 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1806241-263-5 |
| MDL | MFCD09264194 |
| SMILES | O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O |
| InChIKey | BCFGMOOMADDAQU-UHFFFAOYSA-N |
| InChI | InChI=1S/C29H26ClFN4O4S/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/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35) |
| PubChem CID | 208908 |
| Target Point | EGFR |
| Passage | Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| Background | Lapatinib is a potent EGFR and ErbB2 inhibitor. |
| Biological Activity | Lapatinib (formerly GW572016, trade names Tykerb & Tyverb), usually used in the Ditosylate form, is a potent, orally bioavailable dual EGFR/ErbB2 inhibitor with potential anticancer activity. It inhibits epidermal growth factor receptor (EGFR)/ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. It is an FDA approved medication used for the treatment of breast cancer and other solid tumors. Lapatinib acts by reversibly blocking the phosphorylation of EGFR, ErbB2, and the Erk-1 and-2 and AKT kinases. [1] |
| Data Literature Source | [1]. Mol Cancer Ther. 2001 Dec;1(2):85-94; Cancer Res. 2006 Feb 1;66(3):1630-9. [2]. Chefrour M et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Fundam Clin Pharmacol. 2012 Aug;26(4):530-7. [3]. Wainberg ZA，et al. Lapatinib，a dual EGFR and HER2 kinase inhibitor，selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19. [4]. Eryilmaz U，et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418. [5]. 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 |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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