2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Reactive Oxygen Species (ROS) Apoptosis Ferroptosis
  4. anti-TNBC agent-15

anti-TNBC agent-15 是一种铂 (IV) 配合物，具有抗三阴性乳腺癌活性。 anti-TNBC agent-15 抑制癌细胞活力。anti-TNBC agent-15 逆转三阴性乳腺癌细胞对 Cisplatin (HY-17394) 的耐药性，提升细胞内摄取量，通过诱导 DNA 损伤、增加细胞内 ROS 积累并激活线粒体通路，有效触发细胞凋亡 (apoptosis)。 anti-TNBC agent-15 增强脂质过氧化、干扰胱氨酸/谷氨酸转运体-谷胱甘肽过氧化物酶轴信号通路传导，诱导铁死亡 (ferroptosis)。 anti-TNBC agent-15 在三阴性乳腺癌/Cisplatin 异种移植瘤模型中可显著抑制肿瘤生长。 anti-TNBC agent-15 可用于三阴性乳腺癌的研究。

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anti-TNBC agent-15

anti-TNBC agent-15 Chemical Structure

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anti-TNBC agent-15 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

anti-TNBC agent-15 is a platinum (IV) complex with anti-triple-negative breast cancer activity. anti-TNBC agent-15 inhibits cancer cell viability. anti-TNBC agent-15 reverses the resistance of triple-negative breast cancer cells to Cisplatin (HY-17394), increases intracellular uptake, and effectively triggers apoptosis by inducing DNA damage, enhancing intracellular ROS accumulation and activating the mitochondrial pathway. anti-TNBC agent-15 enhances lipid peroxidation, interferes with the signal transduction of the cystine/glutamate transporter-glutathione peroxidase axis, and induces ferroptosis. anti-TNBC agent-15 significantly inhibits tumor growth in triple-negative breast cancer/Cisplatin xenograft models. anti-TNBC agent-15 can be used for the research of triple-negative breast cancer[1].

体外研究
(In Vitro)

anti-TNBC agent-15 (Compound 14) (100 nM-50 μM; 72 h) 可强效抑制 MDA-MB-231、A549、HCT-116、A549/CDDP、MDA-MB-231/CDDP、MCF-10 A 细胞活力，IC50 分别为 2.38、3.77、4.36、4.29、2.25、12.17[1]。
anti-TNBC agent-15 (5 μM; 12-24 h) 显著提高 MDA-MB-231 细胞和 Cisplatin 耐药型 MDA-MB-231/CDDP 细胞中的细胞内铂积累，在 MDA-MB-231/CDDP 细胞中强效诱导 DNA 损伤，升高 γ-H2AX 与 p53 表达水平、彗星实验橄榄尾矩数值[1]。
anti-TNBC agent-15 (5 μM; 24 h) 可通过上调促凋亡蛋白、下调抗凋亡蛋白 Bcl-2 诱导 Cisplatin 耐药的 MDA-MB-231/CDDP 细胞发生凋亡，破坏细胞的线粒体膜电位[1]。
anti-TNBC agent-15 (5 μM; 24 h) 可通过下调 xCT 和 GPX4 的表达，抑制 Cisplatin 耐药 MDA-MB-231/CDDP 细胞中的胱氨酸/谷氨酸转运体-谷胱甘肽过氧化物酶轴[1]。
anti-TNBC agent-15 (5 μM; 24-72 h) 通过铁死亡诱导 Cisplatin 耐药 MDA-MB-231/CDDP 细胞死亡[1]。
anti-TNBC agent-15 (5 μM; 12-24 h) 可破坏 Cisplatin 耐药 MDA-MB-231/CDDP 细胞中的 GSH 氧化还原系统并诱导广泛的脂质过氧化[1]。
anti-TNBC agent-15 (5 μM; 24 h) 抑制 Cisplatin 耐药 MDA-MB-231/CDDP 细胞的迁移与侵袭[1]。

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

anti-TNBC agent-15 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231, A549, HCT-116, A549/CDDP, MDA-MB-231/CDDP, MCF-10 A cells
Concentration: 100 nM, 500 nM, 1 μM, 5 μM, 10 μM, 50
μM
Incubation Time: 72 h
Result: Exhibited the highest cytotoxicity across all tested cell lines, with IC50 values of 2.38 μM (MDA-MB-231), 3.77 μM (A549), 4.36 μM (HCT-116), 4.29 μM (A549/CDDP), 2.25 μM (MDA-MB-231/CDDP), and 12.17 μM (MCF-10 A).
Showed a resistance factor (RF1) of 1.14 (A549/CDDP vs A549) and RF2 of 0.95 (MDA-MB-231/CDDP vs MDA-MB-231), and a selectivity factor (SF) of 5.11 (MCF-10 A vs MDA-MB-231).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231/CDDP cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Induced an apoptotic rate of 52.87% in MDA-MB-231/CDDP cells, which was higher than the rates induced by ligand 8 (22.95%), oxaliplatin (38.4%), and the combination of ligand 8 and oxaliplatin (46.23%).

Western Blot Analysis[1]

Cell Line: MDA-MB-231/CDDP cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Upregulated the expression of pro-apoptotic proteins Cyt c, Bax, cleaved caspase 3, and cleaved caspase 9, with protein densities relative to β-actin reaching ~0.5, ~0.75, ~0.85, and ~0.7, respectively.
Downregulated the expression of anti-apoptotic protein Bcl-2, with a protein density relative to β-actin of ~0.05.\nSignificantly downregulated the expression of cystine/glutamate transporter (xCT) and glutathione peroxidase 4 (GPX4) proteins, with protein densities relative to β-actin reaching ~0.3 and ~0.1, respectively.

Cell Migration Assay [1]

Cell Line: MDA-MB-231/CDDP cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Inhibited the migration and invasion of Cisplatin-resistant MDA-MB-231/CDDP cells
体内研究
(In Vivo)

anti-TNBC agent-15 (5.0-16.7 mg/kg；静脉注射；每 7 天 1 次；共 28 天) 可剂量依赖性地抑制异种移植小鼠中 Cisplatin 耐药三阴性乳腺癌的肿瘤生长，在 16.7 mg/kg 剂量下的肿瘤生长抑制 (TGI) 率为 63.4%，且全身毒性极低[1]。

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

Animal Model: BALB/c-nude (female)[1]
Dosage: 5.0 mg/kg; 16.7 mg/kg
Administration: i.v.; every 7 days; 28 days
Result: Achieved a tumor growth inhibition (TGI) rate of 44.6% at 5.0 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 63.4% at 16.7 mg/kg.
Showed no significant body weight differences compared to saline control during 28-day treatment, indicating low systemic toxicity.
Induced extensive cell nuclear loss in tumors (16.7 mg/kg dose group, H&E staining).
Demonstrated reduced proliferative activity in tumors (16.7 mg/kg dose group, Ki-67 staining).
分子量

1002.31

Formula

C34H39ClN6O13PtS
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

anti-TNBC agent-15 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

anti-TNBC agent-15Reactive Oxygen Species (ROS)ApoptosisFerroptosisanti-TNBC agentapoptosisferroptosisMDA-MB-231 cellsA549 cellsHCT-116 cellsA549/CDDP cellsMDA-MB-231/CDDP cellsMCF-10 A cellstriple-negative breast cancerBALB/c-nude miceInhibitorinhibitorinhibit

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