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Chemical Structure| 586379-66-0 Chemical Structure| 586379-66-0

Structure of PH-797804
CAS No.: 586379-66-0

Chemical Structure| 586379-66-0

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PH-797804 is a pyridinone inhibitor of p38α with IC50 of 26 nM, being 4-fold selective versus p38β and does not inhibit JNK2.

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Product Details of PH-797804

CAS No. :586379-66-0
Formula : C22H19BrF2N2O3
M.W : 477.30
SMILES Code : CNC(=O)C1=CC(N2C(C)=CC(OCC3=C(F)C=C(F)C=C3)=C(Br)C2=O)=C(C)C=C1
MDL No. :MFCD18251426
InChI Key :KCAJXIDMCNPGHZ-UHFFFAOYSA-N
Pubchem ID :22049997

Safety of PH-797804

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

Related Pathways of PH-797804

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • p38β

    p38β, IC50:102 nM

  • p38α

    p38α, IC50:26 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
human small airway epithelial cells 3 µM 4 hours Blocked the SPRBD and SPRBD + IFN-β induced increases in CHST15 and CHST11 expression PMC10866996
human small airway epithelial cells 10 µM 2 hours PH797804 completely blocked the SPRBD-induced increase in phospho-p38 MAPK and inhibited the increased expression of CHST15 and CHST11 PMC10866996

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse PTC53-BCC mouse model Intraperitoneal injection 40 mg/kg Daily for 4 days To evaluate the therapeutic effect of the MKL1 inhibitor CCG-203971 on drug-resistant basal cell carcinoma, results showed that MKL1 inhibitor significantly inhibited tumor growth. PMC5839965

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01314885 Chronic Obstructive Pulmonary ... More >>Disease (COPD) Less << Phase 1 Completed - United Kingdom ... More >> Pfizer Investigational Site London, United Kingdom, SE1 1YR Pfizer Investigational Site Manchester, United Kingdom, M23 9QZ Less <<
NCT00827515 Pain Phase 1 Withdrawn May 2009 -
NCT00383188 Arthritis, Rheumatoid Phase 2 Completed - -
NCT01226693 Healthy Phase 1 Completed - Singapore ... More >> Pfizer Investigational Site Singapore, Singapore, 188770 Less <<
NCT01102660 Osteoarthritis Phase 2 Completed - -
NCT01543919 Pulmonary Disease, Chronic Obs... More >>tructive Less << Phase 2 Completed - -
NCT01479647 Healthy Volunteers Phase 1 Completed - Singapore ... More >> Pfizer Investigational Site Singapore, Singapore, 188770 Less <<
NCT01217918 Healthy Phase 1 Completed - United States, California ... More >> Pfizer Investigational Site Culver City, California, United States, 90232 Pfizer Investigational Site Glendale, California, United States, 91206 Less <<
NCT01924650 Healthy Phase 1 Withdrawn June 2014 -
NCT00620685 Arthritis, Rheumatoid Phase 2 Completed - United States, Arizona ... More >> Pfizer Investigational Site Phoenix, Arizona, United States, 85013 United States, Colorado Pfizer Investigational Site Colorado Springs, Colorado, United States, 80909 United States, Florida Pfizer Investigational Site Miami, Florida, United States, 33169 United States, Maryland Pfizer Investigational Site Frederick, Maryland, United States, 21702 United States, Michigan Pfizer Investigational Site Bingham Farms, Michigan, United States, 48025 Pfizer Investigational Site Kalamazoo, Michigan, United States, 49007 United States, Pennsylvania Pfizer Investigational Site Duncansville, Pennsylvania, United States, 16635 Less <<
NCT02084485 Healthy Phase 1 Completed - United Kingdom ... More >> Pfizer Investigational Site Denmark Hill, London, United Kingdom, SE5 9PJ Less <<
NCT00614705 Neuralgia, Postherpetic Phase 2 Completed - Chile ... More >> Pfizer Investigational Site Vina del Mar, V Region, Chile, 2520997 Russian Federation Pfizer Investigational Site Moscow, Russian Federation, 123098 Pfizer Investigational Site St. Petersburg, Russian Federation, 194175 Pfizer Investigational Site St. Petersburg, Russian Federation, 194354 Pfizer Investigational Site Yaroslavl, Russian Federation, 150030 Spain Pfizer Investigational Site Cadiz, Spain, 11009 Pfizer Investigational Site Madrid, Spain, 28006 Pfizer Investigational Site Ourense, Spain, 32005 Pfizer Investigational Site Sevilla, Spain, 41013 Pfizer Investigational Site Valencia, Spain, 46014 Sweden Pfizer Investigational Site Linkoping, Sweden, 581 85 Pfizer Investigational Site Stockholm, Sweden, 114 54 Pfizer Investigational Site Stockholm, Sweden, 115 22 Ukraine Pfizer Investigational Site Dnipropetrovsk, Ukraine, 49616 Pfizer Investigational Site Donetsk, Ukraine, 83045 Pfizer Investigational Site Kharkiv, Ukraine, 61052 Pfizer Investigational Site Kharkiv, Ukraine, 61068 Pfizer Investigational Site Kharkiv, Ukraine, 61178 Pfizer Investigational Site Kyiv, Ukraine, 04050 Pfizer Investigational Site Odessa, Ukraine, 65025 Pfizer Investigational Site Simferopol, Ukraine, 95006 United Kingdom Pfizer Investigational Site Bexhill on Sea, East Sussex, United Kingdom, TN40 1JJ Pfizer Investigational Site Blackpool, Lancashire, United Kingdom, FY3 7EN Pfizer Investigational Site Weybridge, Surrey, United Kingdom, KT15 2BH Pfizer Investigational Site Solihull, United Kingdom, B91 2JL Less <<
NCT01862887 Healthy Phase 1 Completed - United States, Connecticut ... More >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Less <<
NCT00559910 Chronic Obstructive Pulmonary ... More >>Disease Less << Phase 2 Completed - -
NCT01321463 Pulmonary Disease, Chronic Obs... More >>tructive Less << Phase 2 Completed - -
NCT01589614 Healthy Phase 1 Completed - Singapore ... More >> Pfizer Investigational Site Singapore, Singapore, 188770 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.48mL

2.10mL

1.05mL

20.95mL

4.19mL

2.10mL

References

 

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