Choose Your Country or Region

TAE226 (NVP-TAE226)

Name: TAE226 (NVP-TAE226)
Brand: Selleck Chemicals
SKU: S2820
Rating: 5 (24 reviews)

Catalog No.S2820 Purity: 99.97%

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: 761437-28-9

Selleck's TAE226 (NVP-TAE226) has been cited by 24 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Other FAK Products

Related compound libraries

Choose Selective FAK Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
HCT116 cells	Proliferation assay		48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay, IC50=0.4 μM	25180654
HUVEC	Function assay		72 h	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay, IC50=1 μM	23845217
U87MG cells	Proliferation assay		48 h	Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay, IC50=1.2 μM	25180654
PC3 cells	Proliferation assay		48 h	Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay, IC50=1.6 μM	25180654
MDA-MB-231 cells	Proliferation assay		48 h	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST-1 assay, IC50=2.8 μM	25180654
BT474 cells	Function assay	1 μM	24 h	Induction of apoptosis in human BT474 cells assessed as cleavage of 89 kDa PARP at 1 uM after 24 hrs by Western blotting	18989950
Click to View More Cell Line Experimental Data

Biological Activity

Description

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	Click to View More Targets

In vitro
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 Research	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
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	FAK / p-FAK(Y397) / p-AKT(S473) / AKT / pERK / ERK		31215459
	Growth inhibition assay	Cell viability		21196322

In Vivo
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]
Animal Research	Animal Models	Male nude mice bearing intracranial glioma xenografts
	Dosages	75 mg/kg
	Administration	Administered via oral gavage

References

+ Expand

Chemical lnformation & Solubility

Molecular Weight	468.94	Formula	C₂₃H₂₅ClN₆O₃
CAS No.	761437-28-9	SDF	Download TAE226 (NVP-TAE226) SDF
Smiles	CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 94 mg/mL ( (200.45 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):