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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
Cal27 cells 5 μM 48 hours Evaluate the growth inhibitory effect of PQ401 on Cal27 cells, showing that PQ401 alone inhibits cell growth and acts synergistically with gefitinib Mol Cancer Ther. 2011 Nov;10(11):2124-34.
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 Mol Cancer Ther. 2011 Nov;10(11):2124-34.
Enterococcus faecium 4 μg/ml PQ401 exhibited antimicrobial activity against E. faecium mBio. 2020 Jun 30;11(3):e01140-20.
Vancomycin-resistant S. aureus (VRSA) 4 μg/ml PQ401 exhibited bactericidal activity against VRSA mBio. 2020 Jun 30;11(3):e01140-20.
Methicillin-resistant Staphylococcus aureus (MRSA) 4 μg/ml 4 hours PQ401 exhibited bactericidal activity against MRSA, completely killing bacteria within 4 hours mBio. 2020 Jun 30;11(3):e01140-20.
Antler chondrocytes 10 μM 24 hours PQ401 pretreatment significantly attenuated the rIGF1-induced expression of IHH Cell Cycle. 2017 Mar 19;16(6):522-532.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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 mBio. 2020 Jun 30;11(3):e01140-20.
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. J Biol Chem. 2011 Apr 29;286(17):14983-90
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) Growth Horm IGF Res. 2011 Oct;21(5):285-91

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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