2. Membrane Transporter/Ion Channel Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. P-glycoprotein Apoptosis Bcl-2 Family Reactive Oxygen Species Caspase
  4. Lysosomal P-gp targeted agent 1

Lysosomal P-gp targeted agent 1 (Compound 14) 是一种靶向溶酶体 P-glycoprotein (Pgp) 的抗肿瘤药物。Lysosomal P-gp targeted agent 1 通过过表达的 Pgp 选择性转运到溶酶体，释放一氧化氮生成 reactive oxygen species (ROS)，导致溶酶体膜透化作用 (LMP) 并诱导细胞凋亡 (apoptosis)。Lysosomal P-gp targeted agent 1 能克服 P-glycoprotein 介导的耐药性并导致细胞周期停滞，但对正常细胞的毒性相对较低。Lysosomal P-gp targeted agent 1 具有抗肿瘤活性，可显著抑制肿瘤体积。

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Lysosomal P-gp targeted agent 1 Chemical Structure

Lysosomal P-gp targeted agent 1 Chemical Structure

CAS No. : 3043797-88-9

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Lysosomal P-gp targeted agent 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

Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume[1].

体外研究
(In Vitro)

Lysosomal P-gp targeted agent 1 (48h) 对 MCF-7/ADR 和 A549/Taxol 细胞具有强效的抗多药耐药 (MDR) 活性，对 MCF-7/ADR (IC50 = 0.024 μM) 和 PC-3 细胞 (IC50 = 3.36 μM) 表现出强效的抗肿瘤活性，对耐药性 A549/Taxol 细胞 (IC50 = 1.43 μM) 具有抑制活性和细胞毒性，对 HepG2 细胞 (IC50 = 6.57 μM) 表现出毒性，对 MCF-7 细胞 (IC50 = 21.20 μM) 具有弱抑制活性，对 A549 细胞 (IC50 =23.75 μM) 具有弱抗肿瘤活性，对 MCF10A 细胞 (IC50 = 14.32 μM) 和 BEAS-2B 细胞 (IC50 = 14.80 μM) 表现出低细胞毒性[1]。
Lysosomal P-gp targeted agent 1 (100 μM；24 小时) 在 MCF-7/ADR 中产生的一氧化氮水平高于 MCF-7 细胞，细胞内释放的一氧化氮量与其抗肿瘤活性相关[1]。
Lysosomal P-gp targeted agent 1 (100 nM in MCF-7/ADR, 5 μM in A549/Taxol; 1 小时或3小时) 可以通过过表达的 Pgp 选择性地泵入溶酶体并以时间依赖性方式释放一氧化氮[1]。
Lysosomal P-gp targeted agent 1 (25 nM, 50 nM, 100 nM in MCF-7 and MCF-7/ADR, 1μM, 2 μM, 4 μM in A549, A549/Taxol ; 24 小时) 可作为 Pgp 底物，但不调节 Pgp 表达[1]。
Lysosomal P-gp targeted agent 1 (25-50 nM) 以浓度依赖性方式上调促凋亡蛋白 Bax 的表达，下调抗凋亡蛋白 Bcl-2的表达，诱导 PARP1 的裂解，上调 caspase-3 的表达和 PARP1/Cleaved-PARP1 的比率，诱导 MCF-7/ADR 细胞凋亡[1]。
Lysosomal P-gp targeted agent 1 (10-50 nM; 24 小时) 以剂量依赖性方式使凋亡细胞总数从 8.6% 增加到 65.9%[1]。
Lysosomal P-gp targeted agent 1 (10-50 nM; 12 天) 在 40 和 50 nM 时降低菌落生长，表明其对 MCF-7/ADR 细胞具有长期功效[1]。
Lysosomal P-gp targeted agent 1 (20-40 nM; 24 小时) 干扰 DNA 形成并导致细胞周期停滞[1]。

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

Lysosomal P-gp targeted agent 1 相关抗体:

Apoptosis Analysis[1]

Cell Line: MCF-7/ADR
Concentration: 10, 25, 50 nM
Incubation Time: 24 h
Result: Population of apoptotic cells increased from 8.6 to 65.9% in a dose-dependent manner.
Up-regulated the expression of the pro-apoptotic protein Bax and down-regulated the expression of the anti-apoptotic protein Bcl-2 in a concentration-dependent manner.
Induced the cleavage of PARP1, and up-regulated the expression of caspase-3 and the ratio of PARP1/Cleaved-PARP1.

Cell Proliferation Assay[1]

Cell Line: MCF-7/ADR
Concentration: 10, 20, 40, 50 nM
Incubation Time: 12 d
Result: Significantly reduced colony growth at 40 and 50 nM, demonstrated their long-term efficacy against MCF-7/ADR cells.

Cell Cycle Analysis[1]

Cell Line: MCF-7/ADR
Concentration: 20, 30, 40 nM
Incubation Time: 24 h
Result: The number of cells in the G2/M phase changed from 11.2 to 18.1, 20.3, and 25.3% in dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MCF-7, MCF-7/ADR, A549, A549/Taxol
Concentration: 25 nM, 50 nM, 100 nM in MCF-7 and MCF-7/ADR, 1μM, 2 μM, 4 μM in A549, A549/Taxol
Incubation Time: 24 h
Result: Served as a Pgp substrate but not regulated Pgp expression.
体内研究
(In Vivo)

Lysosomal P-gp targeted agent 1 (1.25-5 mg/kg; 腹腔注射；4 天一次，给药 21 天) 具有抗肿瘤活性，能显著抑制肿瘤体积，且肿瘤倾向于死亡、凋亡或静止，未检测到明显的组织学异常或全身毒性[1]。

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

Animal Model: Female BALB/c nude mice (weighing 18-20 g, 4-5 weeks) (established xenograft model using human MDR cell line A549/Taxol)[1]
Dosage: 1.25, 2.5, 5 mg/kg
Administration: Intraperitoneal injection (i.p.), Once every 4 days for 21 days
Result: Had antitumor activity, significantly inhibited tumor volume (62.7% decrease at 5 mg/kg)
Observed numerous cellular destruction and decreased Ki67 expression in a dose-dependent manner, suggesting that the tumors were inclined to die or become apoptotic or quiescent.
No substantial histological abnormalities or systemic toxicity were detected in the low-, medium-, and high-dose groups.
分子量

706.76

Formula

C39H34N2O9S
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

Lysosomal P-gp targeted agent 1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Lysosomal P-gp targeted agent 13043797-88-9P-glycoproteinApoptosisBcl-2 FamilyReactive Oxygen SpeciesCaspaseP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243MCF-7MCF-7/ADRA549A549/TaxolHepG2PC-3anti-Multidrug resistance (MDR)reactive oxygen species (ROS)Inhibitorinhibitorinhibit

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