Description
Key facts
CAS number:340774-69-8,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:371.4 Da,
Molecular formula:C20H16F3N3O,
PubChem:6398883,
Nature:Synthetic,
Solubility:Soluble in ethanol to 25 mMSoluble in DMSO to 50 mM,
Biochemical name:2-(Pyridin-4-Ylmethylamino)-~{n}-[3-(Trifluoromethyl)phenyl]benzamide,
Biological description:Potent, selective and cell-permeable VEGFR inhibitor (IC50 values are 130, 23 and 18 nM for VEGFR1, 2, and 3 respectively). Inhibits VEGF-induced angiogenesis in vivo. Suppresses hypoxia-induced HIF-1α expression without affecting Akt phosphorylation in vitro.,
Canonical smiles:C1=CC=C(C(=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NCC3=CC=NC=C3,
InChi:InChI=1S/C20H16F3N3O/c21-20(22,23)15-4-3-5-16(12-15)26-19(27)17-6-1-2-7-18(17)25-13-14-8-10-24-11-9-14/h1-12,25H,13H2,(H,26,27),
InChiKey:BLAFVGLBBOPRLP-UHFFFAOYSA-N,
IUPAC Name:2-(pyridin-4-ylmethylamino)-N-[3-(trifluoromethyl)phenyl]benzamide
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.
VEGF Receptor 2 (also known as KDR or Flk-1) VEGF Receptor 1 (Flt-1) c-Kit EGFR ABL1 and PDGFR alpha + beta are receptor tyrosine kinases with significant roles in cell signaling. VEGF Receptor 2 and VEGF Receptor 1 engage with vascular endothelial growth factor assisting in modulating angiogenesis. c-Kit with a known mass of around 145 kDa interacts with stem cell factor facilitating hematopoiesis and melanogenesis. EGFR plays a role in epidermal growth factor signaling influencing cell proliferation. ABL1 weighing about 135 kDa is involved in cell differentiation cell division and stress response. PDGFR alpha and beta located on cell surface membranes respond to platelet-derived growth factors influencing cell growth and division.
Biological function summary
These receptors participate in critical processes such as angiogenesis hematopoiesis and cell proliferation. They often exist as part of receptor-ligand complexes that activate signaling cascades upon ligand binding. VEGF Receptors 1 and 2 are important for blood vessel formation and repair. c-Kit and EGFR impact processes like stem cell maintenance and epithelial cell growth. ABL1 often found in the cytoplasm participates in cellular response to external stimuli. PDGFRs influence connective tissue development contributing to organized cell growth in various tissues.
Pathways
These receptor tyrosine kinases integrate into several key ones including the PI3K/AKT and MAPK/ERK pathways. VEGF Receptor 2 through its activation collaborates with proteins like PI3K and AKT to promote vascular growth and maintenance. c-Kit influences the MAPK/ERK pathway important for cell differentiation through its interaction with proteins such as RAF and MEK. EGFR when activated also engages the MAPK/ERK pathway facilitating epidermal regeneration. ABL1 often interacts within cell cycle control pathways and PDGFRs link to both PI3K/AKT and MAPK/ERK pathways supporting cellular responses to mechanical stresses.
These receptors play roles in cancer and cardiovascular diseases. VEGF Receptors particularly 2 associate with tumor angiogenesis offering pathways that cancer cells exploit for blood supply. EGFR and c-Kit mutations or overexpression often relate to various cancers including non-small cell lung cancer and gastrointestinal stromal tumors. ABL1 when fused with the BCR gene results in chronic myeloid leukemia highlighting its pathological significance. PDGFR alterations can lead to disorders such as glioblastomas. In each case these receptors interact with other signaling proteins such as p53 or Forkhead box proteins emphasizing their broader implications in disease modulation.
