Lapatinib Ditosylate - CAS 388082-77-7
Catalog number: 388082-77-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.
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1.Neratinib Plus Paclitaxel vs Trastuzumab Plus Paclitaxel in Previously Untreated Metastatic ERBB2-Positive Breast Cancer: The NEfERT-T Randomized Clinical Trial.
Awada A1, Colomer R2, Inoue K3, Bondarenko I4, Badwe RA5, Demetriou G6, Lee SC7, Mehta AO8, Kim SB9, Bachelot T10, Goswami C11, Deo S12, Bose R13, Wong A14, Xu F14, Yao B14, Bryce R14, Carey LA15. JAMA Oncol. 2016 Apr 14. doi: 10.1001/jamaoncol.2016.0237. [Epub ahead of print]
Importance: Efficacious ERBB2 (formerly HER2 or HER2/neu)-directed treatments, in addition to trastuzumab and lapatinib, are needed.
2.Characterization of the binding of an anticancer drug, lapatinib to human serum albumin.
Kabir MZ1, Mukarram AK2, Mohamad SB3, Alias Z1, Tayyab S4. J Photochem Photobiol B. 2016 Apr 13;160:229-239. doi: 10.1016/j.jphotobiol.2016.04.005. [Epub ahead of print]
Interaction of a promising anticancer drug, lapatinib (LAP) with the major transport protein in human blood circulation, human serum albumin (HSA) was investigated using fluorescence and circular dichroism (CD) spectroscopy as well as molecular docking analysis. LAP-HSA complex formation was evident from the involvement of static quenching mechanism, as revealed by the fluorescence quenching data analysis. The binding constant, Ka value in the range of 1.49-1.01×105M-1, obtained at three different temperatures was suggestive of the intermediate binding affinity between LAP and HSA. Thermodynamic analysis of the binding data (∆H=-9.75kJmol-1 and ∆S=+65.21Jmol-1K-1) suggested involvement of both hydrophobic interactions and hydrogen bonding in LAP-HSA interaction, which were in line with the molecular docking results. LAP binding to HSA led to the secondary and the tertiary structural alterations in the protein as evident from the far-UV and the near-UV CD spectral analysis, respectively.
3.Ridaforolimus improves the anti-tumor activity of dual HER2 blockade in uterine serous carcinoma in vivo models with HER2 gene amplification and PIK3CA mutation.
Hernandez SF1, Chisholm S2, Borger D3, Foster R4, Rueda BR4, Growdon WB5. Gynecol Oncol. 2016 Apr 1. pii: S0090-8258(16)30083-X. doi: 10.1016/j.ygyno.2016.03.027. [Epub ahead of print]
OBJECTIVE: Uterine serous carcinomas (USC) harbor simultaneous HER2 (ERBB2) over-expression and gain of function mutations in PIK3CA. These concurrent alterations may uncouple single agent anti-HER2 therapeutic efficacy making inhibition of the mammalian target of rapamycin (mTOR) a promising option to heighten anti-tumor response.
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CAS 388082-77-7 Lapatinib Ditosylate

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