2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis Stem Cell/Wnt MAPK/ERK Pathway TGF-beta/Smad Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cytoskeleton
  3. PARP Reactive Oxygen Species (ROS) Apoptosis NF-κB ERK Bcl-2 Family TGF-β Receptor EGFR Cadherin
  4. Theophylline-platinum(IV) prodrug-1

Theophylline-platinum(IV) prodrug-1 是一种 PARP-1 抑制剂。Theophylline-platinum(IV) prodrug-1 可增强 SKOV3-BRCA1-KD 细胞的 DNA 损伤、ROS 产生、线粒体功能障碍、凋亡 (apoptosis) 和 S 期阻滞，同时减少侵袭和转移。Theophylline-platinum(IV) prodrug-1 在 SKOV3-BRCA1-KD 异种移植肿瘤模型中显示出优越的抗肿瘤活性。Theophylline-platinum(IV) prodrug-1 可用于卵巢癌的研究。

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Theophylline-platinum(IV) prodrug-1

Theophylline-platinum(IV) prodrug-1 Chemical Structure

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Theophylline-platinum(IV) prodrug-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in SKOV3-BRCA1-KD cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer[1].

体外研究
(In Vitro)

Theophylline-platinum(IV) prodrug-1 (10-10-10-3 μM, 72 h) 抑制 SKOV3 细胞 (IC50 = 0.13 μM)、SKOV3-BRCA1-KD 细胞 (IC50 = 0.1 μM)、A549 细胞 (IC50 = 0.31 μM)、A549-BRCA1-KD 细胞 (IC50 = 0.18 μM)、MCF-7 细胞 (IC50 = 0.10 μM)、MCF-7-BRCA1-KD 细胞 (IC50 = 0.04 μM)、MDA-MB-231 细胞 (IC50 = 0.08 μM)、IOSE-80 细胞 (IC50 = 0.18 μM) 和 SI 细胞 (IC50 = 18 μM) 的增殖[1]。
Theophylline-platinum(IV) prodrug-1 (10 μM, 6 h) 在 SKOV3 和 SKOV3-BRCA1-KD 细胞中诱导 DNA 损伤[1]。
Theophylline-platinum(IV) prodrug-1 (0.5-2 μM, 24 h) 在 SKOV3 和 SKOV3-BRCA1-KD 细胞中诱导 ROS 产生、线粒体膜电位损伤、细胞周期阻滞和凋亡[1]。
Theophylline-platinum(IV) prodrug-1 (0.5 μM, 24 h) 在 SKOV3 和 SKOV3-BRCA1-KD 细胞中抑制侵袭和转移[1]。

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

Theophylline-platinum(IV) prodrug-1 相关抗体:

Immunofluorescence[1]

Cell Line: SKOV3 and SKOV3-BRCA1-KD cells
Concentration: 0.5, 1, 10 μM
Incubation Time: 6, 24 h
Result: Induced a remarkable 15.13-fold increase in γH2AX foci formation in SKOV3-BRCA1-KD cells.
Showed a 4.45-fold increase in the olive tail moment compared to Cisplatin (HY-17394) in BRCA1-deficient cells.
Resulted in larger and more intense foci, suggesting a more severe and potentially irreparable form of DNA damage.
Induced ROS effects in BRCA1-deficient cells particularly.
Showed the most significant effect on MMP in both cell lines, with the effect being more pronounced in SKOV3-BRCA1-KD cells.

Cell Cycle Analysis[1]

Cell Line: SKOV3 and SKOV3-BRCA1-KD cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Resulted in an S-phase cell proportion of 38.67% in SKOV3 cells and led to an S-phase cell proportion of 63.52% in BRCA1-deficient cells.
Showed S-phase arrest in BRCA1-deficient cells.

Apoptosis Analysis[1]

Cell Line: SKOV3 and SKOV3-BRCA1-KD cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Showed particularly notable apoptosis induction effects in SKOV3 and SKOV3-BRCA1-KD cells.
Exhibited an even more striking effect on SKOV3 cells, inducing apoptosis in 25.7% of the population.

Immunofluorescence[1]

Cell Line: SKOV3 and SKOV3-BRCA1-KD cells
Concentration: 1 μM
Incubation Time: 15 h
Result: Decreased PARP-1 levels in SKOV3-BRCA1-KD cells.
Upregulated γH2AX levels particularly in BRCA1-deficient cancer cells.
Enhanced the pro-apoptotic protein Bax levels and suppressed the antiapoptotic protein Bcl-2 levels.
Downregulated NF-κB, TGF-β, Smad2, EGFR and E-cadherin levels.
Increased the expression of N-cadherin and vimentin.
体内研究
(In Vivo)

Theophylline-platinum(IV) prodrug-1 (Compound 4) (2.5 mg/kg，静脉给药，每三天给药一次，共给药 6 次) 在异种移植 SKOV3-BRCA1-KD 肿瘤模型中表现出卓越的抗肿瘤活性[1]。

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

Animal Model: Female BALB/c-nude mice using a cell-derived xenograft (CDX) SKOV3-BRCA1-KD tumor model[1]
Dosage: 2.5 mg/kg
Administration: i.v. every three days for a total of six doses
Result: Inhibited tumor growth by 71.70%.
Maintained stable body weights.
Showed no significant changes in any of these hematological parameters.
Exhibited a near-normal morphology, similar to that of the control group.
Reduced PARP-1 protein expression.
分子量

792.66

Formula

C25H46Cl2N6O6Pt
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

Theophylline-platinum(IV) prodrug-1 相关分类

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  • 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:

Theophylline-platinum(IV) prodrug-1PARPReactive Oxygen Species (ROS)ApoptosisNF-κBERKBcl-2 FamilyTGF-β ReceptorEGFRCadherinpoly ADP ribose polymerase Nuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesTransforming growth factor beta receptorsEpidermal growth factor receptorErbB-1HER1ROSNF-KBapoptosisovarian cancerSKOV3-BRCA1-KD cellsInhibitorinhibitorinhibit

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