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TAE226 (NVP-TAE226) FAK inhibitor

Name: TAE226 (NVP-TAE226)
Brand: Selleck Chemicals
SKU: S2820
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S2820

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. This compound induces apoptosis.

Chemical Structure

Molecular Weight: 468.94

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
HCT116 cells	Proliferation assay		48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay, IC50=0.4 μM
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
U87MG cells	Proliferation assay		48 h	Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay, IC50=1.2 μM
PC3 cells	Proliferation assay		48 h	Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay, IC50=1.6 μM
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
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	468.94	Formula	C₂₃H₂₅ClN₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	761437-28-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (200.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (21.32mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	PYK2 ^[1] (cell-free assay) 3.5 nM FAK ^[1] (cell-free assay) 5.5 nM Insulin Receptor ^[1] (cell-free assay) 43.5 nM IGF-1R ^[1] (cell-free assay) 140 nM c-Met ^[1] (cell-free assay) 160 nM FLT4 ^[1] (cell-free assay) 220 nM FLT1 ^[1] (cell-free assay) 3.4 μM
In vitro	NVP-TAE226 (< 1 μM) inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr397) in serum-starved U87 cells. This compound (< 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. This chemical (<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. This compound (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. This chemical (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] This compound (5 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. This chemical (<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] This compound (0.1 μM-10 μM) 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] This compound (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. ^[3] This chemical (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. ^[4] It 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/17431114/ [2] https://pubmed.ncbi.nlm.nih.gov/18259944/ [3] https://pubmed.ncbi.nlm.nih.gov/19784551/ [4] http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=40&abstractID=31679 [5] http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=40&abstractID=31680

Applications

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

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