PF-431396 717906-29-1

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Molecular Weight:

506.5 PF-431396 is a dual PYK2/FAK Inhibitor with IC50 of 11 nM and 2 nM, respectively.


Biological Activity


In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced
tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell
spreading. PF-431396 consistently inhibits the increase in protein
tyrosine phosphorylation (PY) induced by the absence of added calcium
and induced by W-7 in the presence of calcium.


Protocol(Only for Reference)


Kinase Assay: [1]

Kinase assays and selectivity profiling

Kinase assays for PYK2 and FAK are determined as followed: unactivated full-length, C-terminal his-tagged human Proteins are used in place of the Src-activated kinase domain protein and that test compounds are preincubated with enzyme for 1 h prior to the addition of 500 μM ATP. IC50 determinations are generated from 8 point dose response curves. Selectivity profiling against a diverse panel of kinases is performed by a commercial vendor and reported as average percent inhibition of duplicate tests.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	506.5
Formula	C22H21F3N6O3S
CAS No.	717906-29-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Chemical Name	N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide

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