2. Apoptosis
  3. Apoptosis
  4. NQO1-responsive prodrug

NQO1-responsive prodrug 是 Gemcitabine (dFdC) (HY-17026) 的前药，具有抗癌作用。NQO1-responsive prodrug 在血浆和肝/肠道 S9 组分中保持稳定，并以 NQO1 依赖的方式释放 dFdC。NQO1-responsive prodrug 可诱导 S 期阻滞和细胞凋亡 (apoptosis)。NQO1-responsive prodrug 在 A549 异种移植小鼠模型中抑制肿瘤生长。NQO1-responsive prodrug 可用于乳腺癌和非小细胞肺癌 (NSCLC) 的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

NQO1-responsive prodrug

NQO1-responsive prodrug Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

NQO1-responsive prodrug 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

NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research[1].

体外研究
(In Vitro)

NQO1-responsive prodrug (compound 2) (72 小时) 对A549细胞 (IC50 = 0.21 μM) 和MCF-7细胞 (IC50 = 0.49 μM) 均表现出抗增殖活性，且对 A549 细胞的选择性高于 L02 细胞，选择性比 (SR) 值为 5.52[1]。
NQO1-responsive prodrug (0.08-0.8 μM，24-36 小时) 以剂量依赖的方式抑制A549细胞的增殖和迁移，在体外显示出优异的抗肿瘤活性，且活性高于dFdC[1]。
NQO1-responsive prodrug (100-400 nM，24 小时) 以剂量依赖的方式诱导 A549 细胞发生 S 期细胞周期阻滞和凋亡[1]。
NQO1-responsive prodrug (300 μM，0-480 分钟) 以 NQO1 依赖的方式释放 dFdC[1]。
NQO1-responsive prodrug 在大鼠血浆和肝/肠 S9 组分中表现出良好的稳定性[1]。
NQO1-responsive prodrug (2 μM，24 小时) 通过在 A549 细胞中产生更少的无活性代谢物 dFdU，并能克服与细胞摄取和脱氨作用相关的耐药机制，从而有效克服了 dFdC 的耐药性[1]。

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

NQO1-responsive prodrug 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 0.08 and 0.8 μM
Incubation Time: 36 h
Result: Resulted in a substantial reduction in colony count at the concentration of 0.08 μM.
Showed a complete suppression of colony formation in A549 cells at 0.8 μM.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 0.2 and 0.8 μM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition of A549 cell migration.
Demonstrated stronger inhibitory effects compared to dFdC at the same concentration (0.8 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 24 h
Result: Induced apoptosis in tumor cells in a concentration-dependent manner.
Induced apoptosis at a concentration of 100 nM with a rate of 10.6 %.
Demonstrated a significantly higher capacity to induce apoptosis than dFdC across the tested concentration range.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 24 h
Result: Dose-dependently induced cell cycle arrest in S phase.
Induced significant S-phase arrest at a much lower concentration (100 nM) than dFdC (400 nM).
体内研究
(In Vivo)

NQO1-responsive prodrug (0.1 和 0.2 mmol/kg，腹腔注射，每周两次，持续 21 天) 在 A549 异种移植小鼠模型中显著减小肿瘤体积，且不影响体重[1]。

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

Animal Model: BALB/c nude mice (3-5 weeks old) subcutaneously injected with A549 cells[1]
Dosage: 0.1 and 0.2 mmol/kg
Administration: i.p., twice a week for 21 days
Result: Effectively inhibited tumor growth at a dose of 0.1 mmol/kg, resulting in a TGI value of 55.0% and a treatment/control ratio (T/C) value of 49.9 %.
Its antitumor activity was significantly enhanced when the dosage was increased from 0.1 mmol/kg to 0.2 mmol/kg, yielding a TGI of 65.8 % and a T/C ratio of 39.1 %.
Showed no significant weight loss.
分子量

658.65

Formula

C32H36F2N4O9
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

NQO1-responsive prodrug 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

NQO1-responsive prodrugApoptosisGemcitabineprodrugdFdCNQO1A549MCF-7breastNSCLCInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
NQO1-responsive prodrug
目录号：
HY-178451
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z