Key Documents

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

Pricing and availability is not currently available.

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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.

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Show Differences

1 of 1

This Item	SML2850	G3545	EPS003
Sigma-Aldrich C7249 CI-1033	Sigma-Aldrich SML2850 Cediranib	Sigma-Aldrich G3545 GW583340 dihydrochloride	Sigma-Aldrich EPS003 CUDC 101
form solid	form powder	form solid	form -
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥97% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level -	Quality Level 100
storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. −20°C
solubility DMSO: >10 mg/mL, H₂O: >10 mg/mL	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 9 mg/mL	solubility DMSO: soluble
Gene Information human ... EGFR(1956), ERBB2(2064), ERBB4(2066)	Gene Information -	Gene Information -	Gene Information -

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

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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

Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.

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

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

A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer.

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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Global Trade Item Number

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

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