TAE226 (NVP-TAE226)

貨號 Cat. No.: S2820
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

TAE226 (NVP-TAE226)

Catalog No.S2820

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.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 403	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 2356	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 3490	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	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.
Targets	FAK	IGF-1R	Pyk2
IC50	5.5 nM	0.14 μM	3.5 nM ^[1]
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]
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]
Features

Protocol(Only for Reference)

Cell Assay: ^[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 Study: ^[1]

Animal Models	Male nude mice bearing intracranial glioma xenografts
Dosages	75 mg/kg
Administration	Administered via oral gavage
Solubility	0.5% methylcellulose, 30 mg/mL

References

Chemical Information

Download TAE226 (NVP-TAE226) SDF

Molecular Weight (MW)	468.94
Formula	C₂₃H₂₅ClN₆O₃
CAS No.	761437-28-9

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	94 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	0.5% methylcellulose,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.