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AB141267

PD 158780, ErbB receptor tyrosine kinase inhibitor

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(1 Publication)

MW 330.18 Da, Purity >99%. Potent ErbB receptor tyrosine kinase inhibitor (IC50 values are 8 μM, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively). Does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest and shows antiproliferative effects in vitro. Active in vivo. Centrally active.

View Alternative Names

Avian erythroblastic leukemia viral (v erb b) oncogene homolog, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, 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, HER1, IMD42, MAP kinase interacting kinase 1, MAP kinase interacting serine/threonine kinase 1, MAP kinase signal-integrating kinase 1, MAP kinase-interacting serine/threonine-protein kinase 1, MAPK signal integrating kinase 1, MGC129539, MITOGEN-ACTIVATED PROTEIN KINASE-INTERACTING SERINE/THREONINE KINASE 1, MKNK1_HUMAN, NISBD2, NR1F3, Nuclear receptor ROR-gamma, Nuclear receptor RZR-gamma, Nuclear receptor subfamily 1 group F member 3, Oncogen ERBB, PIG61, Proto-oncogene c-ErbB-1, RAR related orphan nuclear receptor variant 2, RAR related orphan receptor C, isoform a, RAR related orphan receptor gamma, RAR-related orphan receptor C, RORG_HUMAN, RZR GAMMA, RZRG, Receptor tyrosine-protein kinase ErbB-1, Retinoic acid binding receptor gamma, Retinoid-related orphan receptor-gamma, Rorc, SA7, Species antigen 7, TOR, Urogastrone, Wa5, erb-b2 receptor tyrosine kinase 1, mENA, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2

1 Images
Chemical Structure - PD 158780, ErbB receptor tyrosine kinase inhibitor (AB141267)
  • Chemical Structure

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Chemical Structure - PD 158780, ErbB receptor tyrosine kinase inhibitor (AB141267)

2D chemical structure image of ab141267, PD 158780, ErbB receptor tyrosine kinase inhibitor

Key facts

CAS number

171179-06-9

Purity

>99%

Form

Solid

form

Molecular weight

330.18 Da

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>2</sub>BrN<sub>5</sub>

PubChem

4707

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Soluble in ethanol to 10 mM

Biochemical name

N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine

Biological description

Potent ErbB receptor tyrosine kinase inhibitor (IC50 values are 8 μM, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively). Does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest and shows antiproliferative effects in vitro. Active in vivo. Centrally active.

Canonical smiles

CNC1=NC=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br

InChi

InChI=1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)

InChiKey

KFHMLBXBRCITHF-UHFFFAOYSA-N

IUPAC Name

4-N-(3-bromophenyl)-6-N-methylpyrido[3,4-d]pyrimidine-4,6-diamine

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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
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
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Supplementary information

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

EGFR also known as ErbB-1 or HER1 ROR gamma and MNK1 are proteins involved in significant cellular processes. EGFR is a transmembrane glycoprotein with a molecular weight of approximately 170 kDa and is present in epithelial tissues. ROR gamma is a member of the nuclear receptor family expressed in immune cells particularly in the thymus. MNK1 is a serine/threonine kinase found in various tissues mostly in the cytoplasm but also in the nucleus under stress conditions.
Biological function summary

These proteins function in cellular signaling and gene regulation. EGFR an ErbB receptor dimerizes and activates upon binding its ligand triggering downstream signaling. It is fundamental in processes like cell growth and differentiation. ROR gamma plays an important role in gene expression related to immune functions controlling genes essential for lymphoid organogenesis and T-cell differentiation. MNK1 is involved in the regulation of protein synthesis and responds to extracellular signals to modulate translation.

Pathways

EGFR is part of the MAPK and PI3K/AKT signaling pathways interacting with proteins such as ErbB family members. It impacts processes like cell proliferation and survival. ROR gamma is integral to pathways governing immune response often working alongside other nuclear receptors and cytokines such as IL-17. MNK1 participates in the mitogen-activated protein kinase pathway influencing protein translation through phosphorylation of eukaryotic initiation factor 4E (eIF4E).

EGFR is strongly associated with various cancers including non-small cell lung cancer where its overexpression or mutation leads to increased cell proliferation. It is often a target for ErbB inhibitors which aim to block its signaling. ROR gamma has links to inflammatory diseases such as psoriasis where its role in cytokine production impacts the disease process. MNK1 is associated with neurological disorders due to its influence on protein synthesis affecting neuronal functions when dysregulated.
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Product protocols

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Publications (1)

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

Cancers 10: PubMed30274176

2018

Fenofibrate Interferes with the Diapedesis of Lung Adenocarcinoma Cells through the Interference with Cx43/EGF-Dependent Intercellular Signaling.

Applications

Unspecified application

Species

Unspecified reactive species

Katarzyna Piwowarczyk,Edyta Kwiecień,Justyna Sośniak,Eliza Zimoląg,Emiliana Guzik,Jolanta Sroka,Zbigniew Madeja,Jarosław Czyż
View all publications
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