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TAE226 (NVP-TAE226)

TAE226 (NVP-TAE226)

Item no.	S2820-5000
Manufacturer	Selleckchem
CASRN	761437-28-9
Amount	5 g
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 5 g
Category	Oncology Neuroscience Metabolism Diabetes Cholesterol & Lipid Metabolism Regulation of Appetite Molecular Targets for Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Brain Cancer Nervous System Cancer
Type	Inhibitors
Specific against	other
Smiles	CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	FAK,IGF-1R,Pyk2,FAK
Similar products	NVP-TAE226
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	468, 94
Administration	Administered via oral gavage
Animal Models	Male nude mice bearing intracranial glioma xenografts
Cell lines	U87 and U251 cell lines
Concentrations	10 uM
Dosages	75 mg/kg
Formulation	0.5% methylcellulose
IC50	5.5 nM, 5.5 nM, 5.5 nM, 5.5 nM, 5.5 nM, 5.5 nM
In vitro	NVP-TAE226 (< 1 uM) inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr397) in serum-starved U87 cells. NVP-TAE226 (< 1 uM) also inhibits IGF-I-induced phosphorylation of IGF-1R and activity of its downstream target genes such as MAPK and Akt in both U87 and U251 cells. NVP-TAE226 (<10 uM) retards tumor cell growth and attenuats G(2)-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression in both U87 and U251 cells. NVP-TAE226 (1 uM) inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay in glioma cell lines. NVP-TAE226 (1 uM) treatment of glioma cell lines containing wild-type p53 mainly exhibits G(2)-M arrest, whereas glioma cell lines bearing mutant p53 undergoes apoptosis, as evidence by detection of caspase-3/7 activation and poly(ADP-ribose) polymerase cleavage and by an Annexin V apoptosis assay. [1] NVP-TAE226 (5 uM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 (<10 uM) treatment of the human neuroblastoma cell line SK-N-AS leads to decrease in cellular viability, cell cycle arrest, and an increase in apoptosis. [2] NVP-TAE226 (0.1 uM-10 uM) inhibits tube formation of HMEC1 cells. [3]
In vivo	NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. [1], NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. [3] NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. [4] NVP-TAE226 inhibits 4T1 murine breast tumor growth and metastasis to the lung in a dose-dependent manner in vivo model, associated with inhibition of FAK autophosphorylation at Y397 and Akt phosphorylation at Serine473. [5]
Incubation Time	5 days
Method	Cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2 04 in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyzer.
Solubility (25C)	DMSO 94 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
Chemical Name	Benzamide, 2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-

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