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C7249

卡纽替尼二盐酸盐

Name: 卡纽替尼二盐酸盐
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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产品名称

卡纽替尼二盐酸盐, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

solid

solubility

DMSO: >10 mg/mL, H₂O: >10 mg/mL

storage temp.

−20°C

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

Gene Information

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

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.

Features and Benefits

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.

pictograms

GHS07

signalword

Warning

hcodes

H315,H319,H335

pcodes

P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338

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

新产品

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

0000404996

0000178228

0000139538

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Lapatinib-binding protein kinases in the African trypanosome: identification of cellular targets for kinase-directed chemical scaffolds.

Samiksha Katiyar et al.

PloS one, 8(2), e56150-e56150 (2013-02-26)

Human African trypanosomiasis is caused by the eukaryotic microbe Trypanosoma brucei. To discover new drugs against the disease, one may use drugs in the clinic for other indications whose chemical scaffolds can be optimized via a medicinal chemistry campaign to

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

Cecilia Trinks et al.

Biochemical and biophysical research communications, 393(1), 6-10 (2010-01-26)

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 inhibitor, canertinib (CI-1033)

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

M Sánchez-Martín et al.

International journal of cancer, 131(1), 244-252 (2011-08-10)

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 kinase inhibitors

Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.

Alberto Ocaña et al.

Cancer treatment reviews, 35(8), 685-691 (2009-09-08)

Aberrant activation of HER2 through overexpression has been shown to play an important role in some breast cancers. Therapies against this receptor including the monoclonal antibody, trastuzumab, or the small tyrosine kinase inhibitor, lapatinib have shown to improve the prognosis

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

Chandra P Belani

Cancer investigation, 28(4), 413-423 (2010-03-24)

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 and progress within

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Discover Bioactive Small Molecules for Kinase Phosphatase Biology

全球贸易项目编号

货号	GTIN
C7249-25MG	04061833218075
C7249-5MG	04061833218082

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