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Merck

C7249

CI-1033

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

동의어(들):

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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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C24H25ClFN5O3· 2HCl
CAS 번호:
289499-45-2
Molecular Weight:
558.86
UNSPSC Code:
51111800
PubChem Substance ID:
329775143
NACRES:
NA.77
MDL number:
MFCD09954112

주요 문서

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제품 이름

CI-1033, ≥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)

관련 카테고리

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

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

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

target_organs

Respiratory system

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number
0000404996
0000404996
0000178228
0000178228
0000139538

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문서 라이브러리 방문

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
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)
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
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
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
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