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Chemical Structure| 939791-38-5 Chemical Structure| 939791-38-5

Structure of PF-562271 besylate
CAS No.: 939791-38-5

Chemical Structure| 939791-38-5

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PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with IC50 values of 1.5 nM and 13 nM, respectively.

Synonyms: VS-6062 besylate; PF-562271 (besylate); PF-00562271 Besylate

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Product Details of PF-562271 besylate

CAS No. :939791-38-5
Formula : C27H26F3N7O6S2
M.W : 665.66
SMILES Code : CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O
Synonyms :
VS-6062 besylate; PF-562271 (besylate); PF-00562271 Besylate
MDL No. :MFCD14105612
InChI Key :LKLWTLXTOVZFAE-UHFFFAOYSA-N
Pubchem ID :16118986

Safety of PF-562271 besylate

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

Related Pathways of PF-562271 besylate

RTK
cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NMuMG cells 1 μM Inhibition of FAK activity, blocking the invasion of post-EMT NMuMG cells to EGF PMC3076082
PC3-μM2 cells 0.1 µM to 10 µM 3 hours to 24 hours To study the effect of PF-562271 on PC3-μM2 cell survival, results showed that PF-562271 inhibited FAK phosphorylation and reduced cell survival. PMC4651787
C4-2B4 cells 5 µM To study the effect of PF-562271 on C4-2B4 cell survival, results showed that PF-562271 significantly inhibited the osteocrine-induced cell survival. PMC4651787
human bone marrow-derived MSCs 10 µM 6 hours Inhibited FAK phosphorylation, blocked WSS-induced COX2 and HO-1 expression PMC5548629

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice PCa-118b tumor model Oral gavage 50 mg/kg daily To study the effect of PF-562271 on PCa-118b tumor growth, results showed that PF-562271 alone reduced tumor size, and its combination with cabozantinib further inhibited tumor growth. PMC4651787
Mice 4T1 tumor model Oral Ceritinib 50 mg/kg, Ribociclib 187.5-250 mg/kg Once daily for 49 days To study the inhibitory effect of PF-562271 on 4T1 tumor growth and metastasis PMC2790843
Mice Aortic banding-induced cardiac hypertrophy model Gavage 4 mg/(kg·d) Once daily for 7 days Inhibited FAK/AKT signaling pathway, significantly attenuated the AB-induced hypertrophic response in cADAM23-KO mice PMC6222933
Mice GL261-C57BL/6 mouse glioma implantation model Oral 25 nmol/kg body weight Twice daily for 21 days PF-562271 treatment reversed the upregulation of Pyk2/FAK signaling in recurrent tumors, reduced tumor volume, and increased animal survival. PMC10487692

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.51mL

1.50mL

0.75mL

15.02mL

3.00mL

1.50mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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