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AB282443

Compound 56

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(3 Publications)

MW 388.3 Da, Purity >97%. Cell-permeable, reversible and ATP-competitive, potent and specific inhibitor of tyrosine kinase activity of EGFR.

View Alternative Names

6-bisphosphatase 1, 6-bisphosphate 1-phosphohydrolase 1, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, D fructose 1 6 bisphosphate 1 phosphohydrolase 1, D-fructose-1, EC 3.1.3.11, EGFR_HUMAN, ERBB, ERBB1, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Errp, F16P1_HUMAN, FBP, FBPase 1, Fructose 1 6 bisphosphatase 1, Fructose bisphosphatase 1, Fructose-1, Growth inhibiting protein 17, HER1, Liver fructose bisphosphatase, NISBD2, Oncogen ERBB, PIG61, Proto-oncogene c-ErbB-1, Receptor tyrosine-protein kinase ErbB-1, SA7, Species antigen 7, Urogastrone, Wa5, erb-b2 receptor tyrosine kinase 1, mENA, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2

Key facts

CAS number

171745-13-4

Purity

>97%

Form

Solid

form

Molecular weight

388.3 Da

Molecular formula

C<sub>1</sub><sub>8</sub>H<sub>1</sub><sub>8</sub>BrN<sub>3</sub>O<sub>2</sub>

PubChem

2857

Nature

Synthetic

Solubility

≥16.95mg/mL in DMSO. Insoluble in H2O.

Biochemical name

N-(3-bromophenyl)-6,7-diethoxyquinazolin-4-amine

Biological description

Cell-permeable, reversible and ATP-competitive, potent and specific inhibitor of tyrosine kinase activity of EGFR.

Canonical smiles

CCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OCC

InChi

InChI=1S/C18H18BrN3O2/c1-3-23-16-9-14-15(10-17(16)24-4-2)20-11-21-18(14)22-13-7-5-6-12(19)8-13/h5-11H,3-4H2,1-2H3,(H,20,21,22)

InChiKey

YXOXHAUUTIOBDA-UHFFFAOYSA-N

IUPAC Name

N-(3-bromophenyl)-6,7-diethoxyquinazolin-4-amine

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Product details

For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.
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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
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Supplementary information

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

EGFR also known as Epidermal Growth Factor Receptor and FBP1 or Fructose-16-bisphosphatase 1 plays important roles in different cellular processes. EGFR is a transmembrane glycoprotein and falls within the receptor tyrosine kinases family with a molecular weight of approximately 170 kDa. It is widely expressed in epithelial tissues and involved in cell signaling pathways. FBP1 on the other hand functions as a gluconeogenic enzyme mainly found in the liver and kidney with a molecular weight of about 37 kDa. These proteins each perform distinct roles to maintain proper cellular function.
Biological function summary

EGFR is involved in regulating cell growth differentiation and survival. As part of a signal transduction complex it accommodates ligand binding that triggers dimerization and activation leading to multiple intracellular pathways. FBP1 acts as an important regulator in gluconeogenesis maintaining the balance of glucose production during fasting states. FBP1 does not typically associate with protein complexes in its functionality focusing on the conversion of fructose-16-bisphosphate to fructose-6-phosphate in the cytoplasm.

Pathways

EGFR significantly contributes to the MAPK/ERK and PI3K/AKT signaling pathways which are essential for mediating cellular responses to external growth factors. These pathways connect EGFR with proteins like RAF MEK and AKT which carry out further signaling cascades. FBP1 primarily participates in metabolic pathways and has a more isolated role interacting less with other proteins in these complex signaling networks.

Both EGFR and FBP1 link to specific pathologies. EGFR is often associated with various cancers like non-small cell lung cancer highlighting its role in tumor cell proliferation through interactions with proteins like HER2. Mutations in its gene amplify signaling susceptibility contributing to oncogenesis. On the other hand FBP1 is linked to metabolic disorders such as hypoglycemia due to impaired gluconeogenesis. In these cases reduced enzymatic activity leads to glucose imbalance but it has fewer direct interactions with other proteins in the context of disease states.
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Product protocols

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Publications (3)

Recent publications for all applications. Explore the full list and refine your search

Scientific reports 7:1578 PubMed28484277

2017

Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia.

Applications

Unspecified application

Species

Unspecified reactive species

Brittany M Duggan,Kevin P Foley,Brandyn D Henriksbo,Joseph F Cavallari,Akhilesh K Tamrakar,Jonathan D Schertzer

Clinical cancer research : an official journal of the American Association for Cancer Research 3:2099-106 PubMed9815602

1998

PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner.

Applications

Unspecified application

Species

Unspecified reactive species

M Bos,J Mendelsohn,Y M Kim,J Albanell,D W Fry,J Baselga

Journal of medicinal chemistry 39:267-76 PubMed8568816

1996

Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.

Applications

Unspecified application

Species

Unspecified reactive species

A J Bridges,H Zhou,D R Cody,G W Rewcastle,A McMichael,H D Showalter,D W Fry,A J Kraker,W A Denny
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Complementary Products

Primary Antibodies

AB109732

Anti-FBP1 antibody [EPR4620]

RabMAb|Recombinant

Immunocytochemistry/ Immunofluorescence - Anti-FBP1 antibody [EPR4620] (AB109732)

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Assay Kits

AB273329

Fructose-1,6-Bisphosphatase Activity Assay Kit (Colorimetric)

Functional Studies - Fructose-1,6-Bisphosphatase Activity Assay Kit (Colorimetric) (AB273329)

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Proteins & Peptides

AB286057

Recombinant human FBP1 protein (Active)

SDS-PAGE - Recombinant human FBP1 protein (Active) (AB286057)

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