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C7249

CI-1033

Name: CI-1033
Brand: SIGMA

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

Synonym(s):

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

Empirical Formula (Hill Notation):

C₂₄H₂₅ClFN₅O₃· 2HCl

CAS Number:

289499-45-2

Molecular Weight:

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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Properties

Product Name

CI-1033, ≥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)

Description

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number

0000404996

0000178228

0000139538

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Articles

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

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

Enhanced brain accumulation of pazopanib by modulating P-gp and Bcrp1 mediated efflux with canertinib or erlotinib.

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

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

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

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Global Trade Item Number

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