SBI-581

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SBI-581 

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。

SBI-581

SBI-581 Chemical Structure

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生物活性

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].

IC50 & Target

IC50: 42 nM (TAO3), 237 nM (MEKK3)[1]

体外研究
(In Vitro)

SBI-581 shows moderate selectivity (> 5-10x) against the majority of a broad panel of kinases[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SBI-581 (10 mg/kg, IP, once) displays reasonable pharmacokinetics (t1/2=1.5 hr; AUC= 1202 hr*ng/mL; Cmax= ~2 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

383.44

Formula

C24H21N3O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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