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Chemical Structure| 717906-29-1 Chemical Structure| 717906-29-1

Structure of PF-431396
CAS No.: 717906-29-1

Chemical Structure| 717906-29-1

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PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.

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Product Details of PF-431396

CAS No. :717906-29-1
Formula : C22H21F3N6O3S
M.W : 506.50
SMILES Code : CS(=O)(N(C)C1=CC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O
MDL No. :MFCD16038300
InChI Key :POJZIZBONPAWIV-UHFFFAOYSA-N
Pubchem ID :11598628

Safety of PF-431396

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

Related Pathways of PF-431396

RTK
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • FAK

    PYK2, IC50:11 nM

    FAK, IC50:2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human pulmonary alveolar epithelial cells (HPAEpiCs) 0.1, 1, 3 µM 1 hour Inhibited SiNP-induced COX-2 expression Biomedicines. 2023 Sep 25;11(10):2628.
A20 cells 2.5 µM 1, 2, or 4 hours PF-431396 treatment significantly reduced the ability of A20 cells to spread on fibronectin, indicating that the kinase activities of Pyk2 and FAK are crucial for B cell spreading. J Biol Chem. 2009 Aug 21;284(34):22865-77.
MV4-11 cells 300 nM 16 hours To assess the effect of PF-431396 on the translation rate of proteins in MV4-11 cells, it was found that PF-431396 treatment significantly affected the translation of proteins involved in cell cycle regulation and extracellular matrix organization. Leukemia. 2022 Oct;36(10):2418-2429.
Gastric fundus smooth muscle cells 0.3 µM 2 minutes PDBu or calyculin A contracted gastric fundus smooth muscle strips and increased FAK Y397 phosphorylation in a Ca2+-independent manner J Physiol. 2018 Jun;596(11):2131-2146.
MV4-11 cells 200 nM 24 hours To assess the effect of PF-431396 on the adhesion of MV4-11 cells, it was found that PF-431396 treatment significantly reduced cell adhesion. Leukemia. 2022 Oct;36(10):2418-2429.
A375 melanoma cells 1 µM 24 hours To investigate the effect of PF-431396 on melanoma cell migration and matrix degradation. Results showed that PF-431396 significantly inhibited melanoma cell migration without altering matrix degradation. Cell Death Dis. 2023 Mar 11;14(3):190.
MG6 cells 1000 nM 24 hours To assess the effect of Pyk2 inhibition on MG6 cell proliferation, results showed a significant decrease in proliferation at 1000 nM concentration. J Neuroinflammation. 2024 Aug 6;21(1):196.
HMC3 cells 1000 nM 24 hours To assess the effect of Pyk2 inhibition on HMC3 cell multinucleation, results showed a significant increase in multinucleation at 1000 nM concentration. J Neuroinflammation. 2024 Aug 6;21(1):196.
Caco-2 cells 0.25 µM 24 hours Treatment with PF-43 increased the epithelial barrier function and enhanced mitochondrial respiration levels in Caco-2 cells Tissue Barriers. 2021 Apr 3;9(2):1890526.
H2596 cells 1 µM 48 hours Induced apoptosis, a two-fold increase in the number of apoptotic cells in H2596 cell line Cancer Biol Ther. 2018 Apr 3;19(4):316-327.
MiaPaca 2 cells 1 µM 48 hours Induced apoptosis, significant increase in the number of apoptotic cells in MiaPaca 2 cells Cancer Biol Ther. 2018 Apr 3;19(4):316-327.
Capan 1 cells 2 µM and 4 µM 48 hours Induced apoptosis, significant increase in the number of apoptotic cells in Capan 1 cells Cancer Biol Ther. 2018 Apr 3;19(4):316-327.
Gastric fundus smooth muscle cells 0.3 µM 5 seconds Inhibited EFS-induced gastric fundus smooth muscle contractions and FAK Y397 phosphorylation J Physiol. 2018 Jun;596(11):2131-2146.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats De-endothelialized caudal arterial smooth muscle strips In vitro administration 10 µM 30 minutes PF-431396 inhibited both phasic and tonic components of the K+-induced contractile response and Pyk2 autophosphorylation, indicating that Pyk2 plays an important role in K+-induced contraction. J Biol Chem. 2015 Apr 3;290(14):8677-92

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