BX-320(BX-320) - 药物靶点：PDPK1_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

PDPK1

作用机制

PDK1抑制剂(磷酸肌醇依赖性激酶1抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

Berlex Biosciences

在研机构

Berlex Biosciences

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C23H31BrN8O3

InChIKeyZNSULAZTNWFKEW-UHFFFAOYSA-N

CAS号702676-93-5

关联

100 项与 BX-320 相关的临床结果

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100 项与 BX-320 相关的转化医学

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100 项与 BX-320 相关的专利（医药）

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1

项与 BX-320 相关的文献（医药）

2005-05-01·Journal of Biological Chemistry2区 · 生物学

Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1

2区 · 生物学

Article

作者: Mike Ferrer ; Silke Finster ; Bruno Alicke ; Damian O. Arnaiz ; Dao Lentz ; Sandra L. Biroc ; Marc Adler ; Judi Bryant ; Mark A. Polokoff ; Shendong Yuan ; Daguang Zhu ; James M. Wu ; Harald Dinter ; Brad O. Buckman ; Monica J. Kochanny ; Richard I. Feldman ; Zheng Chang ; Marc Whitlow

The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three potent PDK1 inhibitors, BX-795, BX-912, and BX-320 (IC(50) = 11-30 nm) and their initial biological characterization. The inhibitors blocked PDK1/Akt signaling in tumor cells and inhibited the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis. A number of cancer cell lines with elevated Akt activity were >30-fold more sensitive to growth inhibition by PDK1 inhibitors in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX-320 inhibited the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. The effect of BX-320 on cancer cell growth in vitro and in vivo indicates that PDK1 inhibitors may have clinical utility as anticancer agents.

100 项与 BX-320 相关的药物交易

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