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Chemical Structure| 1276121-88-0 Chemical Structure| 1276121-88-0

Structure of PF-3644022
CAS No.: 1276121-88-0

Chemical Structure| 1276121-88-0

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PF-3644022 is a potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM and Ki = 3 nM). It inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM) and exhibits oral efficacy in acute and chronic inflammatory models.

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Product Details of PF-3644022

CAS No. :1276121-88-0
Formula : C21H18N4OS
M.W : 374.46
SMILES Code : O=C1N[C@H](C)CNC2=C1SC3=CC=C4N=C(C5=CC=C(C)N=C5)C=CC4=C32
MDL No. :MFCD21363374
InChI Key :CMWRPDHVGMHLSZ-GFCCVEGCSA-N
Pubchem ID :44631903

Safety of PF-3644022

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of PF-3644022

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SCC47 (HPV+) 50 µM 48 hours RT increased MK2 protein phosphorylation while MK2 inhibitor alone did the opposite. Dual RT+MK2i treatment prevented RT-induced MK2 phosphorylation. Oncogene. 2019 Nov;38(48):7329-7341
TU167 (HPV−) 50 µM 48 hours RT increased MK2 protein phosphorylation while MK2 inhibitor alone did the opposite. Dual RT+MK2i treatment prevented RT-induced MK2 phosphorylation. Oncogene. 2019 Nov;38(48):7329-7341

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
MMTV-Her2 mice MMTV-Her2 breast cancer model Oral 5 μM 14 days PF3644022 reduced Hsp27-Ser86 phosphorylation and percentage of E-cadherinhigh ducts and increased β-catenin nuclear translocation in mammary glands. PF3644022 did not alter the percentage of ducts with early lesions in mammary glands, but increased the Her2+ eDCCs in blood, bone marrow and lung. Oncogene. 2020 Oct;39(40):6313-6326.
Mice HN009LN (p16−) and HN011T (p16+) PDX models Peritumoral injection 50µM Every other day for a total of 6 injections Dual RT+MK2i treatment significantly decreased tumor volumes and improved animal survival. Oncogene. 2019 Nov;38(48):7329-7341

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.35mL

2.67mL

1.34mL

26.71mL

5.34mL

2.67mL

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

References

 

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