2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. QW-5-70

QW-5-70 是一种靶向秋水仙碱位点的微管蛋白 (tubulin) 抑制剂，可阻断微管蛋白聚合。QW-5-70 可诱导有丝分裂及 G2/M 期细胞周期阻滞，触发线粒体凋亡 (apoptosis)，并抑制癌细胞集落形成与迁移。QW-5-70 可克服由 P-糖蛋白 (P‑glycoprotein) 介导的多药耐药性，同时抑制耐药肿瘤的生长。QW-5-70 在神经母细胞瘤和前列腺癌模型中展现出强大的体外及体内抗肿瘤活性。QW-5-70 可用于高危神经母细胞瘤和去势抵抗性前列腺癌的研究。

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QW-5-70

QW-5-70 Chemical Structure

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QW-5-70 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

QW-5-70 is a potent colchicine‑site tubulin inhibitor that blocks tubulin polymerization. QW-5-70 induces mitotic and G2/M cell cycle arrest, triggers mitochondrial apoptosis, and suppresses cancer cell colony formation and migration. QW-5-70 overcomes P‑glycoprotein‑mediated multidrug resistance and inhibits drug‑resistant tumor growth. QW-5-70 demonstrates strong in vitro and in vivo antitumor efficacy in neuroblastoma and prostate cancer models. QW-5-70 can be used for the research of high-risk neuroblastoma and castration-resistant prostate cancer[1][2].

IC50 & Target[2]

β-Tubulin

 

体外研究
(In Vitro)

QW-5-70 直接与纯化微管蛋白上的秋水仙碱结合位点结合，Kd 为 10.8 μM，抑制微管蛋白聚合，破坏微管网络[1][2]。
QW-5-70 在亲本及耐药性 BE2C/VCR、PC-3/TxR、神经母细胞瘤 (NB) 和前列腺癌细胞中表现出亚纳摩尔级的抗增殖活性，且可规避 P-糖蛋白介导的外排作用[1]。
QW-5-70 可显著降低亲代及耐药的 BE2C/VCR、PC-3/TxR、NB 和前列腺癌细胞的克隆形成能力，抑制其迁移，并诱导 G2/M 期细胞周期阻滞和线粒体凋亡。QW-5-70 与 DFMO (HY-B0744) 或 MLN8237 (HY-10971) 联用时，可增强细胞凋亡并降低克隆形成能力[1][2]。
QW-5-70 可抑制 SK-N-BE (2)-C、BE2C/VCR、PC-3 和 PC-3/TxR 细胞的活力，其 IC50 值分别为 1.0 nM、1.8 nM、1.5 nM 和 1.5 nM[2]。
QW-5-70 (0.1-15 μM) 可使 SK-N-BE (2)-C、NB-1691 和 PC-3 细胞中的微管失稳，表现为聚合态 β-微管蛋白水平降低、可溶性 β-微管蛋白水平升高[2]。
QW-5-70 (2-5 nM) 可诱导 SK-N-BE(2)-C、NB-1691 和 PC-3/TxR 细胞发生 G2/M 期细胞周期阻滞，并导致 BE2C/VCR 和 PC-3/TxR 细胞发生有丝分裂阻滞，同时伴有 p-组蛋白 H3 (Ser10)、细胞周期蛋白 B1 和 p-CDK1 (Thr161) 水平升高。此外，QW-5-70 还可诱导 BE2C/VCR 和 PC-3/TxR 细胞凋亡，表现为 cleaved caspase-3、cleaved PARP 和磷酸化 BCL2 (Ser70) 水平升高，以及总 BCL2 表达降低[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

QW-5-70 相关抗体:

Immunofluorescence[2]

Cell Line: SK-N-BE(2)-C, NB-1691, PC-3 cancer cells
Concentration: 2, 5 nM
Incubation Time: 24 h
Result: Caused disruption of normal microtubule networks in SK-N-BE(2)-C, NB-1691, and PC-3 cells, resulting in fragmented, disorganized microtubule structures compared to untreated control cells.

Western Blot Analysis[2]

Cell Line: BE2C/VCR, PC-3/TxR cancer cells
Concentration: 2, 5 nM
Incubation Time: 24 h
Result: Increased levels of phosphorylated histone H3 (p-Histone H3) and cyclin B1, and reduced levels of phosphorylated CDK1 (p-CDK1 (Thr161)) in BE2C/VCR and PC-3/TxR cells, consistent with induction of mitotic arrest.\n
Increased levels of cleaved caspase-3 (cCas3), cleaved PARP (cPARP), and BCL2-associated X protein (p-BCL2), and reduced levels of B-cell lymphoma 2 (BCL2) in BE2C/VCR and PC-3/TxR cells, consistent with induction of apoptosis.

Cell Viability Assay[2]

Cell Line: SK-N-BE(2)-C neuroblastoma cells
Concentration: 0.125, 0.25, 0.5, 1, 2 nM (QW-5-70 alone)
10, 30, 100, 300, 1000 μM (DFMO alone)
1 nM (QW-5-70) plus 100 mM (DFMO, combination)
Incubation Time: 24 h
Result: Combination treatment with QW-5-70 and DFMO reduced SK-N-BE(2)-C cell viability more effectively than either agent alone.
Increased levels of cleaved PARP compared to single-agent treatment when used at 1 nM plus DFMO at 100 mM, indicating enhanced apoptosis.
Exhibited an additive to synergistic interaction with DFMO as confirmed by synergy analysis.
体内研究
(In Vivo)

QW-5-70 (15, 30 mg/kg；每日给药；连续 14 天) 可显著抑制小鼠体内 Paclitaxel (HY-B0015) 耐药 PC-3/TxR 肿瘤异种移植物的生长[2]。
QW-5-70 (20 mg/kg；每日一次；连续 14 天) 可有效抑制小鼠体内 Vincristine (HY-N0488A) 耐药性 BE2C/VCR 肿瘤异种移植物的生长，且耐受性良好[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

378.38

Formula

C20H18N4O4
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

QW-5-70 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

QW-5-70Microtubule/TubulinApoptosisprostate cancermitotic arrestcolchicine siteG2/M cell cycle arresttubulinP-glycoproteinmicrotubule networksneuroblastomamitochondrial apoptosisBE2C/VCRInhibitorinhibitorinhibit

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