卡纽替尼二盐酸盐

卡纽替尼二盐酸盐结构式
卡纽替尼二盐酸盐结构式
品牌特惠专场
常用名 卡纽替尼二盐酸盐 英文名 Canertinib dihydrochloride
CAS号 289499-45-2 分子量 558.860
密度 1.355g/cm3 沸点 691ºC at 760mmHg
分子式 C24H27Cl3FN5O3 熔点 188-190℃
MSDS 中文版 美版 闪点 371.7ºC
符号 GHS07
GHS07
信号词 Warning

Breast cancer cells can switch between estrogen receptor alpha and ErbB signaling and combined treatment against both signaling pathways postpones development of resistance.

Breast Cancer Res. Treat. 121(3) , 601-13, (2010)

The majority of breast cancers are estrogen responsive, but upon progression of disease other growth promoting pathways are activated, e.g., the ErbB receptor system. The present study focuses on resistance to the pure estrogen antagonist fulvestrant and stra...

A multivariate model of ErbB network composition predicts ovarian cancer cell response to canertinib.

Biotechnol. Bioeng. 109(1) , 213-24, (2012)

Identifying the optimal treatment strategy for cancer is an important challenge, particularly for complex diseases like epithelial ovarian cancer (EOC) that are prone to recurrence. In this study we developed a quantitative, multivariate model to predict the ...

Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.

Int. J. Cancer 131(1) , 244-52, (2012)

Deregulation of ErbB/HER receptor tyrosine kinases has been linked to several types of cancer. The mechanism of activation of these receptors includes establishment of receptor dimers. Here, we have analyzed the action of different small molecule HER tyrosine...

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.

Bioorg. Med. Chem. Lett. 18(22) , 5916-9, (2008)

Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ten other protein kinases including all...

The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.

Cancer Invest. 28(4) , 413-23, (2010)

Reversible epidermal growth factor receptor tyrosine kinase inhibitors are often used for the treatment of non-small cell lung cancer following failure of cytotoxic chemotherapy. While these agents are active in a subset of patients, most develop resistance a...

The pan-ErbB receptor tyrosine kinase inhibitor canertinib induces ErbB-independent apoptosis in human leukemia (HL-60 and U-937) cells.

Biochem. Biophys. Res. Commun. 393(1) , 6-10, (2010)

Epidermal growth factor (EGF) receptor tyrosine kinase inhibitors have recently been shown to display anti-neoplastic effects in human malignant myeloid cells. Our study was initiated in order to determine the effect of the pan-ErbB receptor tyrosine kinase i...

Rationale and clinical results of multi-target treatments in oncology.

Int. J. Biol. Markers 22(1 Suppl 4) , S77-87, (2007)

During the last 10 years, the concept of targeted biological therapy for the treatment of cancer has emerged. Targeted agents entered clinical practice only recently, and the first drugs with demonstrated clinical efficacy were mainly inhibitors of the ErbB f...

Pharmacology of epidermal growth factor inhibitors.

Int. J. Biol. Markers 22(1 Suppl 4) , S24-39, (2007)

Research into the molecular bases of malignant diseases has yielded the development of many novel agents with potential antitumor activity. Evidence for a causative role for the epidermal growth factor receptor (EGFR), which is now regarded as an excellent ta...

Suppression of proliferation of two independent NF1 malignant peripheral nerve sheath tumor cell lines by the pan-ErbB inhibitor CI-1033.

Cancer Biol. Ther. 7(12) , 1938-46, (2008)

Neurofibromatosis Type 1 (NF1) is characterized by the abnormal proliferation of neuroectodermal tissues and the development of certain tumors, particularly neurofibromas, which may progress into malignant peripheral nerve sheath tumors (MPNSTs). Effective ph...

The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo.

Biochem. Biophys. Res. Commun. 414(3) , 563-8, (2011)

The ErbB receptor family has been suggested to constitute a therapeutic target for tumor-specific treatment of malignant melanoma. Here we investigate the effect of the pan-ErbB tyrosine kinase inhibitor canertinib on cell growth and survival in human melanom...