PND-1186 (VS-4718) 1061353-68-1

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Molecular Weight:

501.5 PND-1186 (VS-4718) is a reversible and selective FAK Inhibitor with IC50 of 1.5 nM. Phase 1.


Biological Activity


In vitro, PND-1186 inhibits 4T1 breast carcinoma motility, promotes 4T1
Apoptosis in suspended conditions, and decreases 4T1 soft agar colony
number and size. In HEY and OVCAR8 cells, VS-4718 promotes G0-G1
cell-cycle arrest followed by cell death.


In mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1
subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8
tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma
tumor growth inhibition.


Protocol(Only for Reference)


Kinase Assay: [1]

In vitro kinase activity

GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 µM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophometic color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.

Cell Assay: [1]

Cell lines	Murine ID8 ovarian carcinoma cells
Concentrations	~1 μM
Incubation Time	6 days
Method	For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5?04 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times.

Animal Study: [1]

Animal Models	Mice bearing ID8 tumors or 4T1 tumors
Formulation	polyethylene glycol 400 (PEG400) in PBS (1:1) for s.c.; 5% sucrose for p.o.
Dosages	100 mg/kg every 12 hours for s.c.; 0.5 mg/mL for p.o.
Administration	s.c. or p.o.

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)	501.5
Formula	C25H26F3N5O3
CAS No.	1061353-68-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	SR-2156

Chemical Name	2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide

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