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Chemical Structure| 194423-15-9 Chemical Structure| 194423-15-9

Structure of PD168393
CAS No.: 194423-15-9

Chemical Structure| 194423-15-9

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PD168393 is an inhibitor that targets EGFR with IC50 of 0.70 nM irreversibly. It is not active against insulin, PDGFR, FGFR and PKC.

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Product Details of PD168393

CAS No. :194423-15-9
Formula : C17H13BrN4O
M.W : 369.22
SMILES Code : C=CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O
MDL No. :MFCD02179207
InChI Key :HTUBKQUPEREOGA-UHFFFAOYSA-N
Pubchem ID :4708

Safety of PD168393

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PD168393

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    EGFR, IC50:0.70 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDM) 10 μmol/L 30 minutes Inhibited LPS-induced EGFR phosphorylation Protein Cell. 2020 Feb;11(2):144-149.
Malignant peripheral nerve sheath tumor cells (MPNST cells) 2 μM 24-48 hours To assess the effects of PD168393 on MPNST cell survival, caspase activation, and autophagy. PD168393 induced a cytostatic response accompanied by suppression of Akt and mTOR activation and increased autophagic activity. Neuro Oncol. 2012 Mar;14(3):266-77.
BT-474 breast cancer cells 100 nM 60 minutes PD168393 inhibited phosphorylation of PLCγ1 and Stat1 in BT-474 cells. Proc Natl Acad Sci U S A. 2006 Jun 27;103(26):9773-8.
NIH 3T3 cells 100 nM 60 minutes PD168393 showed rapid and potent inhibition of Her2-induced tyrosine phosphorylation with half-maximal inhibition at ~100 nM. Proc Natl Acad Sci U S A. 2006 Jun 27;103(26):9773-8.
Spinal cord astrocytes 10 μM, 20 μM, 40 μM 6, 12, 24, 48, 72 hours PD168393 significantly inhibited scratch-induced reactive astrogliosis and proinflammatory cytokine/mediator secretion of reactive astrocytes. J Neuroinflammation. 2014 Apr 5;11:71.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Adult female Sprague-Dawley rats T10 contusion model Local administration 2 mM 0.5 μl/h for 14 days Local administration of PD168393 suppressed CSPGs production and glial scar formation in the injured area, resulting in reduced demyelination and neuronal loss, which correlated with significant improvement in hindlimb motor function and bladder function in SCI rats. J Neuroinflammation. 2014 Apr 5;11:71.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.08mL

5.42mL

2.71mL

References

 

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