NVP-TAE 226 (Synonyms: TAE226)

Name: NVP-TAE 226
Brand: MedChemExpress
SKU: HY-13203
Rating: 5.0 (12 reviews)

Cat. No.: HY-13203 Purity: 99.77%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC₅₀s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC₅₀s of 3.5 nM and 44 nM, respectively.

For research use only. We do not sell to patients.

NVP-TAE 226 Chemical Structure

CAS No. : 761437-28-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 12 publication(s) in Google Scholar

10 Publications Citing Use of MCE NVP-TAE 226

: NVP-TAE 226 purchased from MedChemExpress. Usage Cited in: Patent. US20170285005A1.; TAE226 reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes.

: NVP-TAE 226 purchased from MedChemExpress. Usage Cited in: Patent. US20150175695A1.; The small molecule inhibitor for FAK, TAE226, reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes. A) Podocytes are cultured on placental laminin in the presence or absence of TAE226 overnight. Extracts are prepared and analyzed by western blot for expression of pFAK397 and total FAK. FAK activation is also analyzed by western blot of podocyte extracts from stretched and non-stretched cells, demonstrating that biomechanical stretching directly activates

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 5.5 nM (FAK), 3.5 nM (Pyk2), 140 nM (IGF-IR), 40 nM (InsR), 0.16 μM (c-Met), 0.36 μM (KDR), 0.48 μM (Flt3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	IC₅₀	8.3 μM Compound: TAE-226	Cytotoxicity against human A172 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A172 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
A375P	GI₅₀	1.69 μM Compound: TAE226	Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
A498	IC₅₀	0.81 μM Compound: TAE226	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 34111829]
A549	IC₅₀	1.02 μM Compound: 1; TAE-226	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
A549	IC₅₀	1.16 μM Compound: TAE-226	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
A549	IC₅₀	1.31 μM Compound: 1; TAE-226	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35486993]
ASPC1	IC₅₀	4.82 μM Compound: 1; TAE226	Antiproliferative activity against human ASPC1 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
ASPC1	IC₅₀	6.73 μM Compound: 1; TAE226	Antiproliferative activity against human AsPC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human AsPC1 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
ASPC1	IC₅₀	6.73 μM Compound: 1; TAE226	Antiproliferative activity against human AsPC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human AsPC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
ASPC1	IC₅₀	6.73 μM Compound: TAE226	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay	[PMID: 29102081]
BXPC-3	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
BXPC-3	IC₅₀	1.03 μM Compound: 1; TAE226	Antiproliferative activity against human BxPC3 cells after 72 hrs by CCK8 assay Antiproliferative activity against human BxPC3 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
BXPC-3	IC₅₀	1.03 μM Compound: TAE226	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 29102081]
CAKI-1	IC₅₀	1.05 μM Compound: TAE226	Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 34111829]
HCT-116	IC₅₀	0.23 μM Compound: TAE226	Inhibition of colony formation in human HCT116 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human HCT116 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
HCT-116	GI₅₀	0.27 μM Compound: TAE226	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
HCT-116	IC₅₀	0.29 μM Compound: 2; TAE226	Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
HCT-116	IC₅₀	0.39 μM Compound: TAE-226	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by WST1 assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by WST1 assay	[PMID: 28284808]
HCT-116	IC₅₀	0.4 μM Compound: TAE226	Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
HK-2	IC₅₀	8.2 μM Compound: TAE-226	Cytotoxicity against human HK2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HK2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 31923858]
HK-2	IC₅₀	8.2 μM Compound: 1; TAE-226	Cytotoxicity against human HK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
HUVEC	IC₅₀	1 μM Compound: TAE-226	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay	[PMID: 23845217]
KM3/BTZ	IC₅₀	4.386 μM Compound: 1; TAE226	Antiproliferative activity against bortezomib- resistant human KM3/BTZ cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against bortezomib- resistant human KM3/BTZ cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
L02	IC₅₀	5.212 μM Compound: 1; TAE226	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
L02	IC₅₀	5.37 μM Compound: 1; TAE226	Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
L02	IC₅₀	5.37 μM Compound: 1; TAE226	Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
MCF-10A	IC₅₀	8.76 μM Compound: 2; TAE226	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MCF7	IC₅₀	0.45 μM Compound: 2; TAE226	Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MDA-MB-231	GI₅₀	1.49 μM Compound: TAE226	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
MDA-MB-231	IC₅₀	1.9 μM Compound: TAE226	Inhibition of colony formation in human MDA-MB-231 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human MDA-MB-231 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
MDA-MB-231	IC₅₀	2.8 μM Compound: TAE226	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST-1 assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
MDA-MB-231	IC₅₀	4.06 μM Compound: TAE-226	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
MDA-MB-231	IC₅₀	4.24 μM Compound: 1; TAE-226	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
MIA PaCa-2	IC₅₀	5.23 μM Compound: 1; TAE226	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
NCI/ADR-RES	IC₅₀	> 5 μM Compound: 1; TAE226	Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
NCI-H1975	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
NCI-H1975	IC₅₀	> 2 μM Compound: 1; TAE226	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
PANC-1	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human PANC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
PANC-1	IC₅₀	> 20 μM Compound: 1; TAE226	Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
PANC-1	IC₅₀	> 20 μM Compound: TAE226	Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay	[PMID: 29102081]
PC-3	IC₅₀	0.26 μM Compound: TAE226	Inhibition of colony formation in human PC3 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human PC3 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
PC-3	IC₅₀	1.21 μM Compound: 2; TAE226	Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
PC-3	IC₅₀	1.6 μM Compound: TAE226	Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
Raji	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human Raji cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
Sf9	IC₅₀	6.79 nM Compound: 1; TAE226	Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo assay Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo assay	[PMID: 30978560]
U-251	IC₅₀	6.3 μM Compound: TAE-226	Cytotoxicity against human U251 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human U251 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
U-87MG ATCC	IC₅₀	0.19 μM Compound: TAE226	Inhibition of colony formation in human U87MG cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human U87MG cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
U-87MG ATCC	IC₅₀	1.2 μM Compound: TAE226	Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay	[PMID: 25180654]
U-87MG ATCC	IC₅₀	1.3 μM Compound: TAE-226	Cytotoxicity against human U87MG cells assessed as reduction in cell viability by WST1 assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability by WST1 assay	[PMID: 28284808]
U-87MG ATCC	IC₅₀	1.58 μM Compound: 2; TAE226	Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
U-87MG ATCC	IC₅₀	1.67 μM Compound: TAE-226	Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
U-87MG ATCC	IC₅₀	2.9 μM Compound: TAE-226	Cytotoxicity against human U-87 MG cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human U-87 MG cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
U-87MG ATCC	EC₅₀	41 nM Compound: 41	Inhibition of JNK in human U87MG cells overexpressing EGFR V3 mutant assessed as inhibition of c-jun phosphorylation after 6 hrs by ELISA Inhibition of JNK in human U87MG cells overexpressing EGFR V3 mutant assessed as inhibition of c-jun phosphorylation after 6 hrs by ELISA	10.1039/C1MD00219H

In Vitro

NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC₅₀ range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr³⁹⁵). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G₂-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr¹⁵) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G₂-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

468.94

Formula

C₂₃H₂₅ClN₆O₃

CAS No.

761437-28-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C=CC=C1)NC2=NC(NC3=C(C=C(C=C3)N4CCOCC4)OC)=NC=C2Cl)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 11.11 mg/mL (23.69 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1325 mL	10.6623 mL	21.3247 mL
5 mM	0.4265 mL	2.1325 mL	4.2649 mL
10 mM	0.2132 mL	1.0662 mL	2.1325 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.11 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.11 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 1.11 mg/mL (2.37 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 1.11 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (7.10 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (10.66 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) LCMS (123 KB)

Handling Instructions (2659 KB)

References

[1]. Liu TJ, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007, 6(4), 1357-1367. [Content Brief]

[2]. Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083. [Content Brief]

[3]. Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3(11):e3800. [Content Brief]

Cell Assay ^[1]	Glioma 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 analyzer. The antiproliferative activity of NVP-TAE 226 (ranging from 0.25 to 1 μM) on cells growing in culture is determined using a tetrazolium-based colorimetric MTT assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Male nude mice used for this study are 6 to 8 weeks old. In DMEM/F12 serum-free media (5 μL), 5×10⁵ of U87 cells and 1×10⁶ of LN229 cells per mouse are implanted intracranially through a guide-screw system. Four days after injection of the tumor cells, mice are randomized into three groups for each cell line (n=6). Mice in group 1 are treated with 50 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose, via an oral gavage. The mice in group 2 receive 75 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose. The mice in group 3 the same vehicle used for administration of NVP-TAE 226 (control). Treatment frequency is once a day for 5 days and off for 2 days, for a duration of 4 weeks. Mice are monitored daily. Mice are euthanized when they are moribund, and the whole brain is extracted for rapid freezing in liquid nitrogen and storage at -70°C. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Liu TJ, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007, 6(4), 1357-1367. [Content Brief] [2]. Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083. [Content Brief] [3]. Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3(11):e3800. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1325 mL	10.6623 mL	21.3247 mL	53.3117 mL
	5 mM	0.4265 mL	2.1325 mL	4.2649 mL	10.6623 mL
	10 mM	0.2132 mL	1.0662 mL	2.1325 mL	5.3312 mL
	15 mM	0.1422 mL	0.7108 mL	1.4216 mL	3.5541 mL
	20 mM	0.1066 mL	0.5331 mL	1.0662 mL	2.6656 mL

NVP-TAE 226 Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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NVP-TAE 226761437-28-9TAE226TAE 226TAE-226FAKPyk2IGF-1RInsulin ReceptorApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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NVP-TAE 226 (Synonyms: TAE226)

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NVP-TAE 226 Related Antibodies

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NVP-TAE 226 Related Antibodies

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NVP-TAE 226 Related Classifications

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