Abcam, ab141267, PD 158780, ErbB receptor tyrosine kinase inhibitor

Size: 10mg / 50mg
MW 330.18 Da, Purity >99%. Potent ErbB receptor tyrosine kinase inhibitor (IC 50 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 G 1 cell cycle arrest and shows antiproliferative effects in vitro . Active in vivo. Centrally active.
Key facts
CAS number:171179-06-9,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:330.18 Da,
Molecular formula:C14H12BrN5,
PubChem:4707,
Nature:Synthetic,
Solubility:Soluble in DMSO to 50 mMSoluble 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

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

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.