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Merck
CN

C7249

CI-1033

≥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

Key Documents

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Product Name

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)

Related Categories

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

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
0000404996
0000178228
0000178228
0000139538

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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
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
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
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
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
View All Related Papers

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