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Merck
CN
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安全信息

C7249

Sigma-Aldrich

卡纽替尼二盐酸盐

≥98% (HPLC)

别名:

Canertinib dihydrochloride, N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide dihydrochloride, N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride, PD183805

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About This Item

经验公式（希尔记法）:
C24H25ClFN5O3· 2HCl
CAS号:
289499-45-2
分子量:
558.86
MDL编号:
MFCD09954112
UNSPSC代码:
51111800
PubChem化学物质编号:
329775143
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

solid

溶解性

DMSO: >10 mg/mL
H2O: >10 mg/mL

储存温度

−20°C

SMILES字符串

Cl.Cl.Fc1ccc(Nc2ncnc3cc(OCCCN4CCOCC4)c(NC(=O)C=C)cc23)cc1Cl

InChI

1S/C24H25ClFN5O3.2ClH/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16;;/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29);2*1H

InChI key

JZZFDCXSFTVOJY-UHFFFAOYSA-N

基因信息

human ... EGFR(1956) , ERBB2(2064) , ERBB4(2066)

生化/生理作用

CI-1033 is a potent, irreversible ATP binding site–directed pan-ErbB tyrosine kinase inhibitor with IC50 in the low nanomolar range for EGFR, HER2, and ErbB-4.
CI-1033 is a potent, irreversible pan-erbB tyrosine kinase inhibitor.

特点和优势

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the EGFR page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H315,H319,H335

危险分类

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000404996
0000404996
0000178228
0000178228
0000139538

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Hesham A M Gomaa et al.
International journal of genomics, 2018, 7628734-7628734 (2018-11-15)
To investigate and examine the reversal effects of canertinib on the activity of EGFR and tamoxifen resistance in drug-resistant human breast carcinoma cells (MCF-7/TamR). The antiproliferative activity of canertinib alone or in combination with a conventional EGFR-targeting chemotherapies cytotoxic drugs
Kristen N Richards et al.
Cancer, 116(13), 3233-3243 (2010-06-22)
ERBB receptor tyrosine kinases can mediate proliferation, migration, adhesion, differentiation, and survival in many types of cells and play critical roles in many malignancies. Recent reports suggest a role for EGFR signaling in proliferation and survival of neuroblastoma, a common
Cecilia Trinks et al.
Biochemical and biophysical research communications, 410(3), 422-427 (2011-06-15)
Canertinib is a novel ErbB-receptor inhibitor currently in clinical development for the treatment of solid tumors overexpressing ErbB-receptors. We have recently demonstrated that canertinib displays anti-proliferative and pro-apoptotic effects in human myeloid leukemia cells devoid of ErbB-receptors. The mechanism mediating
Emelie A Djerf Severinsson et al.
Biochemical and biophysical research communications, 414(3), 563-568 (2011-10-11)
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 melanoma cells in
Mukul Minocha et al.
International journal of pharmaceutics, 436(1-2), 127-134 (2012-06-13)
Primary objective of this investigation was to delineate the differential impact of efflux transporters P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) on brain disposition and plasma pharmacokinetics of pazopanib. In addition, this research investigated whether inhibition of these efflux
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