PF-562271 717907-75-0

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Molecular Weight:

507.49 PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.


Biological Activity


PF-562271 binds in the ATP-binding cleft of FAK, forming two of the
three [canonical" H-bonds between the inhibitor and main-chain atoms in
the kinase hinge region. PF-562271 is potent in an inducible cell-based
assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM)
results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks
bFGF-stimulated blood vessel Angiogenesis as performed in chicken
chorioallantoic membrane assays. PF-262271 potently blocks blood vessel
sprouting without detectable changes in vascular leakage. PF-562271
(250 nM) results in complete inhibition of collective A431 cell invasion
into collagen gels.


PF-562271 ( PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of
the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.)
results in altered E-cadherin dynamics in mice, which correlates with
reduced E-cadherin–dependent collective cell movement. PF-562271 (25
mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6
subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg,
oral) results in significant and similar increases in osteocalcin and
cancellous bone parameters and a decrease in tumor growth and signs of
bone healing in rats implanted with MDA-MB-231 cells in the tibia.


Protocol(Only for Reference)


Kinase Assay: [1]

Recombinant kinase assay

Purified-activated FAK kinase domain (410–689 aa) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2 for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 mol/L H2SO4). IC50 values are determined using the Hill-Slope Model.

Animal Study: [1]

Animal Models	Athymic female mice bearing BxPc3 or PC3-M xenografts.
Formulation	5% Gelucire
Dosages	50 mg/kg
Administration	Oral gavage
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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)	507.49
Formula	C21H20F3N7O3S
CAS No.	717907-75-0

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

Solubility (25°C) *	In vitro	DMSO	101 mg/mL (199.01 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-

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Product Categories : Angiogenesis > FAK Inhibitor