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4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline; N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-propenamide, PD 168393
C17H13BrN4O
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 25 mg/mL, clear
storage temp.
room temp
SMILES string
C=CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O
InChI
1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)
InChI key
HTUBKQUPEREOGA-UHFFFAOYSA-N
Application
PD168393 has been used in the acute inhibition of ErbB4.
Biochem/physiol Actions
PD168393 is a 6-acrylamido-4-anilinoquinazoline compound. It increases apoptosis in malignant peripheral nerve sheath tumor cells, stimulated by lysosomal dysfunction.
PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2. PD168393 has an IC50 value of 0.70 nM for EGFR, and is inactive against insulin, PDGFR, FGFR and PKC.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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Neuron, 98(2), 380-393 (2018-04-10)
Top-down attention is crucial for meaningful behaviors and impaired in various mental disorders. However, its underpinning regulatory mechanisms are poorly understood. We demonstrate that the hippocampal-prefrontal synchrony associates with levels of top-down attention. Both attention and synchrony are reduced in
Dynamic ErbB4 Activity in Hippocampal-Prefrontal Synchrony and Top-Down Attention in Rodents
Neuron, 98(2), 380-393 (2018)
The pan erbB inhibitor PD168393 enhances lysosomal dysfunction-induced apoptotic death in malignant peripheral nerve sheath tumor cells.
Neuro-Oncology, 14(3), 266-277 (2012)
Cell death & disease, 9(9), 877-877 (2018-08-31)
Many stress conditions including chemotherapy treatment is known to activate Src and under certain condition Src can induce the apoptotic signal via c-Jun N-terminal kinase (JNK) activation. Here we report that the newly synthesized β-phenylacrylic acid derivatives, MHY791 and MHY1036
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