2. Apoptosis Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Apoptosis DNA/RNA Synthesis Reactive Oxygen Species (ROS) Keap1-Nrf2
  4. QD 232

QD 232 是一种喹唑啉二酮类 ROS 诱导剂和凋亡 (apoptosis) 诱导剂，具有细胞毒性、氧化还原调节作用。QD 232 可促进 ROS 积累，激活 NRF2 介导的氧化应激应答和未折叠蛋白应答通路，上调下游抗氧化及应激应答基因。QD 232 可抑制 HSP2 和 LSP 启动子驱动的 mtDNA 转录，破坏线粒体氧化磷酸化功能。QD 232 可诱导胰腺导管腺癌细胞凋亡，对 Gemcitabine (HY-17026) 耐药的胰腺导管腺癌细胞产生细胞毒性。QD 232 可延缓小鼠胰腺癌异种移植模型中的肿瘤生长。

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QD 232

QD 232 Chemical Structure

CAS No. : 1527467-32-8

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QD 232 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

QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model[1].

体外研究
(In Vitro)

QD 232 (30 nM-10 μM; 72 h) 可抑制 MIA PaCa-2、Panc-1 和 BxPC-3 胰腺导管腺癌 (PDAC) 细胞系的增殖，其 IC50 值分别为 2.3 μM、0.9 μM 和 5.2 μM[1]。
QD 232 (30 nM-10 μM; 72 h) 可抑制 Gemcitabine (HY-17026) 耐药型 MIA PaCa-2-GR 细胞及正常 HPDE 胰腺细胞的增殖，IC50 值分别为 3.6 μM 和 4.5 μM[1]。
QD 232 (30 nM-10 μM; 72 h) 在 MIA PaCa-2 细胞中的增殖抑制作用会被 5 mM NAC (HY-B0215) 预处理所减弱[1]。
QD 232 处理可在 MIA PaCa-2、Panc-1 和 BxPC-3 细胞中诱导 CHOP 和 GRP78 蛋白水平呈时间依赖性升高，在 MIA PaCa-2 和 BxPC-3 细胞中上调 HO-1 蛋白，且不会在 MIA PaCa-2 和 BxPC-3 细胞中诱导 NQO1 蛋白表达[1]。

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

QD 232 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MIA PaCa-2, Panc-1, BxPC-3 pancreatic ductal adenocarcinoma (PDAC) cell lines
Concentration: 30 nM - 10 μM
Incubation Time: 72 h
Result: Inhibited cell proliferation with IC50 values of 2.3 μM in MIA PaCa-2 cells, 0.9 μM in Panc-1 cells, and 5.2 μM in BxPC-3 cells.

Cell Proliferation Assay[1]

Cell Line: gemcitabine-resistant MIA PaCa-2-GR PDAC cell line and HPDE normal pancreatic cell line
Concentration: 30 nM - 10 μM
Incubation Time: 72 h
Result: Inhibited cell proliferation with an IC50 of 3.6 μM in MIA PaCa-2-GR cells and 4.5 μM in HPDE cells.

Cell Proliferation Assay[1]

Cell Line: MIA PaCa-2 PDAC cell line
Concentration: 30 nM - 10 μM; 5 mM NAC (pretreatment)
Incubation Time: 72 h
Result: Attenuated the proliferation inhibitory effect of QD 232 when cells were pretreated with 5 mM NAC, though protection was not complete.
体内研究
(In Vivo)

QD 232 (20 mg/kg；给药 5 天/停药 2 天循环；共 31 天) 在 6 周龄 NOD/SCID 小鼠的 MIA PaCa-2 胰腺导管腺癌异种移植模型中实现 65% 的肿瘤生长抑制[1]。

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

Animal Model: NOD/SCID mice with Pancreatic ductal adenocarcinoma (6-week-old)[1]
Dosage: 20 mg/kg
Administration: 5 days on/two days off cycles; 31 days
Result: Suppressed tumor growth by 65% over the 31-day study period.
分子量

293.28

Formula

C16H11N3O3
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

QD 232 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

QD 2321527467-32-8QD232QD-232ApoptosisDNA/RNA SynthesisReactive Oxygen Species (ROS)Keap1-Nrf2Panc-1unfolded protein responsemtDNA transcriptionapoptosispancreatic ductal adenocarcinomaHPDE pancreatic cellsBxPC-3MIA PaCa-2-GRMIA PaCa-2NRF2-mediated oxidative stress responseInhibitorinhibitorinhibit

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