TAE226 (NVP-TAE226) - Moligand™, 10mM in DMSO , Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta, CAS No.761437-28-9, Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
TAE226 (NVP-TAE226) - Moligand™, 10mM in DMSO , Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta, CAS No.761437-28-9, Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
TAE226 (NVP-TAE226) 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 . 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. 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. NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells.
In vivo
NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. 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. Cell Data
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.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
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