SBI-581是一种口服有效的选择性的丝氨酸苏氨酸激酶 TAO3 抑制剂，IC50 值为 42 nM。SBI-581 促进 RAB11 阳性囊泡中 TKS5α 的积累。SBI-581 抑制侵袭性伪足形成。SBI-581 在小鼠腹腔注射后的药代动力学较为合理。SBI-581 具有抗肿瘤活性。
货号:ajcx38264
CAS:N/A
分子式:C24H21N3O2
分子量：383.44
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.