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.
Targets
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)
Click to View More Targets
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
HUVEC MoLKSpVv[3Srb36gZZN{[Xl? NHrsXIE4OiCq NWnRSIRDSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgbY4hUFWYRVOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDWSWdHNXO2aX31cIF1\WRicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgW3NVNTFiYYPzZZktKEmFNUC9NUDPxE1? MW[yN|g1PTJzNx?=
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>
Assay
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
Formula

C23H25ClN6O3

CAS No. 761437-28-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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