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Chemical Structure| 196868-63-0 Chemical Structure| 196868-63-0

Structure of PQ401
CAS No.: 196868-63-0

Chemical Structure| 196868-63-0

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PQ401, a selective insulin-like growth factor-1 receptor blocker, is a diarylurea compound that inhibits IGF1R autophosphorylation with IC50 < 1 μM.

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Product Details of PQ401

CAS No. :196868-63-0
Formula : C18H16ClN3O2
M.W : 341.79
SMILES Code : O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=CC(Cl)=CC=C3OC
MDL No. :MFCD00160558
InChI Key :YBLWOZUPHDKFOT-UHFFFAOYSA-N
Pubchem ID :9549305

Safety of PQ401

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PQ401

RTK

Isoform Comparison

Biological Activity

Target
  • IGF-1R

    IGF-1R, IC50:<1 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Enterococcus faecium 4 μg/ml PQ401 exhibited antimicrobial activity against E. faecium PMC7327171
Vancomycin-resistant S. aureus (VRSA) 4 μg/ml PQ401 exhibited bactericidal activity against VRSA PMC7327171
Cal27 cells 5 μM 48 hours MYCi975 inhibited proliferation, invasion, and migration of CAL27 cells. PMC3213311
Pinctada fucata oocytes 10^-11 to 10^-6 M 30 minutes To investigate the dose-dependent effect of hrIGF-I on MAPK phosphorylation, results showed that hrIGF-I induced a dose-dependent phosphorylation of p44/42 MAPK at concentrations ranging from 10−11 to 10−7 M. PMC4766514
Pinctada fucata oocytes 10^-7 M 0, 5, 10, 60, 180, and 360 minutes To investigate the dose-dependent effect of hrIGF-I on MAPK phosphorylation, results showed that hrIGF-I induced a dose-dependent phosphorylation of p44/42 MAPK at concentrations ranging from 10−11 to 10−7 M. PMC4766514
Methicillin-resistant Staphylococcus aureus (MRSA) 4 μg/ml 4 hours PQ401 exhibited bactericidal activity against MRSA, completely killing bacteria within 4 hours PMC7327171
SCC-25 cells 5 μM 48 hours Evaluate the growth inhibitory effect of PQ401 on SCC-25 cells, showing that PQ401 alone inhibits cell growth and acts synergistically with gefitinib PMC3213311
Antler chondrocytes 10 μM 24 hours PQ401 pretreatment significantly attenuated the rIGF1-induced expression of IHH PMC5384582

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Pinctada fucata Pearl oyster Intramuscular injection 0.06 μg/g body weight Single injection, lasting for 3 hours To investigate the effect of hrIGF-I on glycogen metabolism, results showed that hrIGF-I stimulated the PI3K and MAPK pathways to increase glycogen levels in digestive glands and adductor muscles, and decrease glucose levels in hemocytes. PMC4766514
Caenorhabditis elegans MRSA infection model Liquid medium 5 μg/ml 5 days PQ401 at 5 μg/ml completely prevented C. elegans death caused by MRSA infection PMC7327171
Mice C57BL/6J mice and NIRKO mice POA injection 10 ng Single injection, monitored for 6 hours To investigate the inhibitory effect of PQ401 on IGF-1-induced hyperthermia. Results showed that pretreatment with PQ401 significantly attenuated the IGF-1-induced increase in core body temperature and BAT temperature. PMC3083203
Non-obese diabetic (NOD) female mice Type 1 diabetic mouse model Intraperitoneal injection 50 mg/kg Three times a week for 3 weeks To investigate the effects of PQ401 on diabetic kidney disease parameters, results showed PQ401 had no significant effects on diabetic state (hyperglycemia, weight loss) or renal disease parameters (hypertrophy, hyperfiltration and albuminuria) PMC4238882

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.63mL

2.93mL

1.46mL

29.26mL

5.85mL

2.93mL

References

 

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