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Chemical Structure| 1144035-53-9 Chemical Structure| 1144035-53-9

Structure of PF-8380
CAS No.: 1144035-53-9

Chemical Structure| 1144035-53-9

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PF-8380 is a potent and specific autotaxin inhibitor with IC50 of 2.8 nM.

4.5 *For Research Use Only !

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Product Details of PF-8380

CAS No. :1144035-53-9
Formula : C22H21Cl2N3O5
M.W : 478.33
SMILES Code : O=C(N1CCN(CCC(C2=CC=C3NC(OC3=C2)=O)=O)CC1)OCC4=CC(Cl)=CC(Cl)=C4
MDL No. :MFCD20527274
InChI Key :JMSUDQYHPSNBSN-UHFFFAOYSA-N
Pubchem ID :25265312

Safety of PF-8380

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335-H413
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PDE

    Autotaxin, IC50:2.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
EHEB cells 16 μM and 32 μM 24 h PF-8380 exerts therapeutic potential by inhibiting CLL cell survival and cell cycle, enhancing apoptosis and chemosensitivity. PMC11681649
MEC-1 cells 16 μM and 32 μM 24 h PF-8380 exerts therapeutic potential by inhibiting CLL cell survival and cell cycle, enhancing apoptosis and chemosensitivity. PMC11681649
SCC cells 1 μM Inhibit ATX activity and evaluate its effect on cell proliferation PMC10770346
LR-MSCs 1 µM 30 min PF-8380 significantly reduced the migration rates of FOXF1-silenced LR-MSCs, with levels comparable to scrambled control siRNA transfected LR-MSCs PMC7718269
U87-MG 1 μM 45 min Decreased clonogenic survival, reduced migration and invasion, attenuated radiation-induced Akt phosphorylation PMC3775313
GL261 1 μM 45 min Decreased clonogenic survival, reduced migration and invasion, attenuated radiation-induced Akt phosphorylation PMC3775313
Bone marrow derived macrophages (BMDMs) 10 µM 6 h To assess the effect of PF8380 on macrophage inflammatory response, results showed that PF8380 treatment significantly reduced the TNF-α/IL-10 ratio, indicating attenuated inflammatory response. PMC7744112

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice SCC tumor model Oral 30 mg/kg Twice daily, starting from day +10 Evaluate the effect of PF-8380 on SCC tumor growth, finding that PF-8380 initially prevents tumor growth but then the tumor burden progressively reaches that of untreated mice PMC10770346
Mice PRG-1-/- mice and PRG-1R346T mice Intraperitoneal injection 30 mg/kg Single dose, lasting 3 hours PF-8380 reduced cortical hyperexcitability and restored behavioral phenotypes in PRG-1-/- and PRG-1R346T mice by inhibiting ATX activity. PMC6153268
Mouse GL261 heterotopic tumor model Intraperitoneal injection 10 mg/kg Once daily for five consecutive days Delayed tumor growth, reduced tumor vascularity PMC3775313
Mice Myocardial infarction model Intraperitoneal injection 10 mg/kg Twice daily for 7 days To evaluate the effect of PF8380 on post-myocardial infarction inflammatory response, results showed that PF8380 significantly reduced the inflammatory response, improved cardiac functional recovery, reduced scar size and enhanced angiogenesis. PMC7744112

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.05mL

20.91mL

4.18mL

2.09mL

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