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Merck
CN

C7249

卡纽替尼二盐酸盐

≥98% (HPLC), ErbB tyrosine kinase inhibitor, solid

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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关于此项目

经验公式（希尔记法）:
C24H25ClFN5O3· 2HCl
化学文摘社编号:
289499-45-2
分子量:
558.86
UNSPSC Code:
51111800
PubChem Substance ID:
329775143
NACRES:
NA.77
MDL number:
MFCD09954112

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产品名称

卡纽替尼二盐酸盐, ≥98% (HPLC)

SMILES string

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

assay

≥98% (HPLC)

form

solid

solubility

DMSO: >10 mg/mL
H2O: >10 mg/mL

storage temp.

−20°C

Quality Level

100

Gene Information

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

相关类别

Features and Benefits

This compound is featured on the EGFR page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
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.

Biochem/physiol Actions

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.

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

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

target_organs

Respiratory system

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000404996
0000404996
0000178228
0000178228
0000139538

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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
Melkon Iradyan et al.
Cancers, 11(8) (2019-08-04)
Targeting epidermal growth factor receptor (EGFR) with tyrosine kinase inhibitors (TKI) has been widely exploited to disrupt aberrant phosphorylation flux in cancer. However, a bottleneck of potent TKIs is the acquisition of drug resistance mutations, secondary effects, and low ability
Amanda Nordigården et al.
British journal of haematology, 155(2), 198-208 (2011-08-19)
Recent findings have indicated that tyrosine kinase inhibitors (TKIs) targeting the ERBB receptor family display anti-leukaemic effects, despite the lack of receptor expression on human leukaemic cells. The occurrence of activating mutations in the gene encoding FMS-like tyrosine kinase 3
Olivier Rixe et al.
Cancer chemotherapy and pharmacology, 64(6), 1139-1148 (2009-03-19)
To evaluate the efficacy and safety of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in metastatic breast cancer (MBC). Patients with measurable, progressive, or recurrent MBC whose primary tumor expressed > or =1 ErbB receptor were randomized to the following CI-1033
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