JavaScript is disabled in your browser. Please enable JavaScript to view this website.
AB141402

Canertinib (CI-1033), EGFR and HER2/ErbB2 tyrosine kinase inhibitor

Be the first to review this product! Submit a review

|

(0 Publication)

MW 558.9 Da, Purity >99%. Potent, irreversible pan-ErbB tyrosine kinase inhibitor (IC50 values are 1.5 and 9 nM at EGFR and ErbB2 respectively). Orally active. Antitumor and radiation-sensitizing agent. Active in vivo and in vitro.
1 Images
Chemical Structure - Canertinib (CI-1033), EGFR and HER2/ErbB2 tyrosine kinase inhibitor (AB141402)
  • Chemical Structure

Lab

Chemical Structure - Canertinib (CI-1033), EGFR and HER2/ErbB2 tyrosine kinase inhibitor (AB141402)

2D chemical structure image of ab141402, Canertinib (CI-1033), EGFR and HER2/ErbB2 tyrosine kinase inhibitor

Key facts

CAS number

289499-45-2

Purity

>99%

Form

Solid

form

Molecular weight

558.9 Da

Molecular formula

C<sub>2</sub><sub>4</sub>H<sub>2</sub><sub>7</sub>Cl<sub>3</sub>FN<sub>5</sub>O<sub>3</sub>

PubChem

156413

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

Canertinib dihydrochloride

Biological description

Potent, irreversible pan-ErbB tyrosine kinase inhibitor (IC50 values are 1.5 and 9 nM at EGFR and ErbB2 respectively). Orally active. Antitumor and radiation-sensitizing agent. Active in vivo and in vitro.

Canonical smiles

C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl.Cl

InChi

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

InChiKey

JZZFDCXSFTVOJY-UHFFFAOYSA-N

IUPAC Name

N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;dihydrochloride

style
left-column

Complementary Products

Proteins & Peptides

AB310794

Recombinant Human ErbB2 / HER2 protein

HPLC - Recombinant Human ErbB2 / HER2 protein (AB310794)

  • 0
  • 0
Primary Antibodies

AB214275

Anti-ErbB2 / HER2 antibody [EPR19547-12]

RabMAb|Recombinant

Immunocytochemistry/ Immunofluorescence - Anti-ErbB2 / HER2 antibody [EPR19547-12] (AB214275)

  • 5
  • 3
Assay Kits

AB283881

Human ErbB2 / HER2 ELISA Kit

Recombinant|SimpleStep

Sandwich ELISA - Human ErbB2 / HER2 ELISA Kit (AB283881)

  • 0
  • 0
Biochemicals

AB142139

RepSox, TGF-beta type 1 receptor inhibitor

Chemical Structure - RepSox, TGF-beta type 1 receptor inhibitor (AB142139)

  • 0
  • 0
style
left-column

Product details

This product is manufactured by BioVision, an Abcam company and was previously called 1617 Canertinib (CI-1033, PD-183805). 1617-50 is the same size as the 50 mg size of ab141402.
style
left-column

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
style
left-column

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

ErbB2 also known as HER2 is a receptor tyrosine kinase with a mass of approximately 185 kDa. HER2 belongs to the epidermal growth factor receptor (EGFR) family which includes EGFR itself ErbB3 and ErbB4 (HER4). These proteins exist on the cell surface and participate in cell signaling processes. HER2 is widely expressed in many tissues notably in epithelial cells of the gastrointestinal tract breast and respiratory system. The receptor does not need a ligand to activate and often forms heterodimers especially with other members of the EGFR family.
Biological function summary

HER2 regulates cell growth survival and differentiation by activating several signaling pathways. Though it possesses kinase activity HER2 often functions as part of a heterodimeric receptor complex enhancing its kinase signaling capability when paired with ErbB3. The receptor complex transduces signals from extracellular to intracellular environments playing an essential role in cellular processes that determine cell fate and tissue development.

Pathways

HER2 is a significant component of the MAPK/ERK and PI3K/AKT signaling cascades. These pathways regulate cell proliferation and survival. HER2 interacts with proteins like Grb2 and PI3K which are critical for downstream signaling in these pathways. These interactions enable the transmission of signals that influence aspects of the cell cycle metabolism and anti-apoptotic mechanisms.

HER2 has a well-established link to breast and gastric cancers. Overexpression or amplification of the HER2 gene correlates with aggressive tumor growth and poor prognosis. HER2 interacts with proteins such as EGFR which can also contribute to oncogenic signaling. Treatments targeting HER2 like the ErbB2 inhibitor Canertinib have been developed to block its activity and are important in the management of HER2-positive cancers.
style
left-column
style
left-column

Product protocols

style
left-column
style
left-column
style
right-column

Product promise

We are committed to supporting your work with high-quality reagents, and we're here for you every step of the way. In the unlikely event that one of our products does not perform as expected, you're protected by our Product Promise.
For full details, please see our Terms & Conditions

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com