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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NamePF-431396
SynonymsPF431396
PF-431396
PF-431396 hydrate
N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide
N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide

Synonyms

PF431396
PF-431396
PF-431396 hydrate
N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide
N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
N-[2-[[[2-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]phenyl]-N-MethylMethanesulfonaMide
N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]-N-methyl-Methanesulfonamide hydrate
N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide PF-431396
CAS717906-29-1
EINECS
Chemical FormulaC22H21F3N6O3S
Molecular Weight506.5
inchi
Package10 mM * 1 mL;5 mg;10 mg;50 mg;100 mg
PriceEmail to quote
DescriptionsPF-431396

PF-431396

MedChemExpress (MCE)

HY-10460

717906-29-1

99.13%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US

Descriptions

PF-431396

PF-431396

MedChemExpress (MCE)

HY-10460

717906-29-1

99.13%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US
may vary elsewhere.

PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.

PF-431396 has a Kd value of 445 nM for BRD4[2]. PF-431396 appeares to selectively inhibit BCR-induced tyrosine phosphorylation of Pyk2 and FAK[3]. PF-431396 (2.5, 5 μM, 45 min) inhibits the phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs[3].

PF-431396 (10 or 30 mg/kg, orally) prevents bone loss induced by estrogen deficiency in rats primarily by stimulating bone formation, providing independent pharmacological confirmation for the function of PYK2 in regulating bone formation[4].

IC50: 2 nM (FAK)
11 nM (PYK2)[1]. Kd: 445 nM (BRD4)[1]. Cellular Effect Cell Line Type Value Description References

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[1]. Seungil Han, et al. Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem. 2009 May 8
284(19): 13193–13201.
[Content Brief]

[2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [Content Brief]

[3]. Tse KW, et al. B cell receptor-induced phosphorylation of Pyk2 and focal adhesion kinase involves integrins and the Rap GTPases and is required for B cell spreading. J Biol Chem. 2009 Aug 21
284(34):22865-77.
[Content Brief]

[4]. Leonard Buckbinder, et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc Natl Acad Sci U S A. 2007 Jun 19
104(25):10619-24.
[Content Brief]

Supplier Websitehttps://www.medchemexpress.com/PF-431396.html
Last Update2025-05-21 16:50:25
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