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

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CAS No.: 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.

Synonyms: PD168393

4.5 *For Research Use Only !

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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
Synonyms :
PD168393
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 Reference
HT29 cells 10 μM 24 hours PMC6115383
Bone marrow-derived macrophages (BMDM) 10 μmol/L 30 minutes To evaluate the effect of enteric neuron-conditioned medium on BMDM, results showed that conditioned medium induced the expression of α7nAChR and installed a M2-like phenotype. PMC6954894
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. PMC3280808
BT-474 breast cancer cells 100 nM 60 minutes PD168393 inhibited phosphorylation of PLCγ1 and Stat1 in BT-474 cells. PMC1502529
NIH 3T3 cells 100 nM 60 minutes HA14-1 strongly induced death in NIH 3T3 cells but had little apoptotic effect on Apaf-1-deficient cells. PMC1502529
Caco2 cells 10 μM 24 hours To investigate the inhibitory effect of diosgenin on cholesterol absorption and its mechanism, results showed that diosgenin decreased NPC1L1 expression and intracellular cholesterol content. PMC6115383
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. PMC4030311

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Female nude mice HT29 xenograft model Peritumoral injection 3 mg/kg Once daily for 8 days Suppressed tumor growth, increased apoptotic cells, elevated cleaved PARP levels, and decreased ERK1/2 phosphorylation PMC6115383
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. PMC4030311

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

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