TAE226 (NVP-TAE226)

Catalog No.S2820

For research use only.

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.

TAE226 (NVP-TAE226) Chemical Structure

CAS No. 761437-28-9

Selleck's TAE226 (NVP-TAE226) has been cited by 22 publications

Purity & Quality Control

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Biological Activity

Description 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.
PYK2 [1]
(cell-free assay)
FAK [1]
(cell-free assay)
Insulin Receptor [1]
(cell-free assay)
IGF-1R [1]
(cell-free assay)
c-Met [1]
(cell-free assay)
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3.5 nM 5.5 nM 43.5 nM 140 nM 160 nM
In vitro

NVP-TAE226 (< 1 μM) inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr397) in serum-starved U87 cells. NVP-TAE226 (< 1 μM) 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 μM) 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 μM) 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 μM) 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 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 (<10 μM) 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 μM-10 μM) inhibits tube formation of HMEC1 cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells M3PiV3Bzd2yrZnXyZZRqd25iYYPzZZk> NXTkdVlCPDhiaB?= M3XWSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME2wMlQh|ryP M4O0b|I2OThyNkW0
U87MG cells NYf0cmtoWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmDnOFghcA>? NIHOPZZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGW4O21IKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME2xMlIh|ryP MnfLNlUyQDB4NUS=
PC3 cells MlLiVJJwdGmoZYLheIlwdiCjc4PhfS=> MYG0PEBp MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:OS54IN88US=> MWeyOVE5ODZ3NB?=
MDA-MB-231 cells M1zoV3Bzd2yrZnXyZZRqd25iYYPzZZk> MYm0PEBp M3;yXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA1QCCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:Oi56IN88US=> M2jrPVI2OThyNkW0
BT474 cells M1ntOWZ2dmO2aX;uJIF{e2G7 MlzxNUDPxE1? M1LPSVI1KGh? NUfGbGRVUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDCWFQ4PCClZXzsd{Bie3Onc4Pl[EBieyClbHXheoFo\SCxZjC4PUBsTGFiUFHSVEBifCBzIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6p NXWzSlAyOTh7OEm5OVA>
Methods Test Index PMID
Western blot FAK / p-FAK(Y397) / p-AKT(S473) / AKT / pERK / ERK 31215459
Growth inhibition assay Cell viability 21196322
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]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: U87 and U251 cell lines
  • Concentrations: 10 μM
  • Incubation Time: 5 days
  • Method: Cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 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 analyze
Animal Research:[1]
  • Animal Models: Male nude mice bearing intracranial glioma xenografts
  • Dosages: 75 mg/kg
  • Administration: Administered via oral gavage

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 468.94


CAS No. 761437-28-9
Storage 3 years -20°C powder
2 years -80°C in solvent

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Tech Support

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Handling Instructions

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