SBI-581 |
Catalog No.GC64771 |
SBI-581 es un potente inhibidor selectivo de la serina-treonina quinasa TAO3 activo por vÍa oral, con una IC50 de 42 nM. SBI-581 promueve la acumulaciÓn de TKS5α en vesÍculas positivas para RAB11. SBI-581 inhibe la formaciÓn de invadopodios. SBI-581 muestra una farmacocinética razonable en ratones mediante inyecciÓn IP. SBI-581 muestra actividad antitumoral.
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Sample solution is provided at 25 µL, 10mM.
SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity[1].
SBI-581 shows moderate selectivity (> 5-10x) against the majority of a broad panel of kinases[1].
SBI-581 (10 mg/kg, IP, once) displays reasonable pharmacokinetics (t1/2=1.5 hr; AUC= 1202 hr*ng/mL; Cmax= ~2 μM)[1].
[1]. Iizuka S, et al. Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth. Cancer Res. 2021 Mar 15;81(6):1472-1485.
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