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  4. (rac)-ZK-304709

(rac)-ZK-304709是ZK-304709的一种异构体。它是一种首创的口服多靶点肿瘤生长抑制剂，能抑制多种细胞周期依赖性激酶(Cdks)、血管内皮生长因子受体激酶(VEGF-RTKs)和血小板源性生长因子受体激酶β(PDGF-RTKβ)。(rac)-ZK-304709能够剂量依赖性地抑制神经内分泌肿瘤(NET)细胞的增殖和集落形成。它通过诱导G2期细胞周期阻滞和细胞凋亡来直接作用于NET细胞，同时降低MCL1、survivin和HIF1α的表达。在原位BON肿瘤模型中，(rac)-ZK-304709可使原发肿瘤生长减少80%，并降低肿瘤微血管密度。这些结果表明，(rac)-ZK-304709通过诱导细胞凋亡和抑制肿瘤诱导的血管生成来有效控制肿瘤生长，可能成为抑制NET的潜在试剂。

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(rac)-ZK-304709 Chemical Structure

(rac)-ZK-304709 Chemical Structure

CAS No. : 1010440-84-2

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(rac)-ZK-304709 相关抗体

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生物活性

(rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.

分子量

444.96

Formula

C22H29ClN6O2
CAS 号
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.
纯度 & 产品资料
参考文献

(rac)-ZK-304709 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

(rac)-ZK-3047091010440-84-2OthersInhibitorinhibitorinhibit

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