2. Others Apoptosis Cell Cycle/DNA Damage
  3. Drug Derivative Apoptosis CDK ASK1
  4. MG16

MG16 是 10-Methoxycamptothecin (HY-N0446) 前药。MG16 可下调 CDK6、上调 ASK1 的表达。MG16 可诱导细胞周期阻滞、凋亡 (Apoptosis)。MG16 对 Lewis 肺癌、小细胞肺癌、非小细胞肺癌表现出抗癌活性。

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MG16

MG16 Chemical Structure

CAS No. : 2349329-01-5

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MG16 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer[1].

IC50 & Target[1]

CDK6

 

体外研究
(In Vitro)

MG16 (48 h) 可在体外强效抑制 LLC、A549 和 H446 肺癌细胞的增殖，IC50 分别为 408.2 ± 32.4、613.1 ± 54.7 及 140.4 ±
10.4 nM[1]。
MG16 (0.1-100 nM; 48 h) 处理 48 h 后可在 A549 和 H446 肺癌细胞中诱导剂量依赖性凋亡，在两种细胞系中的促凋亡活性均显著强于 SN-38[1]。
MG16 (对于 A54，90.1-1 μM, 对于 H446，10-100 nM; 24 h) 可调控关键凋亡蛋白的表达，并在处理 24 h 后于 A549 和 H446 肺癌细胞中诱导强烈的 Caspase-3 活化，其 Caspase-3 活化作用比 SN-38 更显著[1]。
MG16 (613.1 nM; 48 h) 可在其 IC50 浓度下处理 A549 肺癌细胞 48 h 后诱导细胞周期阻滞于 G0/G1 期[1]。

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

MG16 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 lung cancer cells, H446 lung cancer cells
Concentration: 0.1-1 μM (A549 cells); 10-100 nM (H446 cells)
Incubation Time: 24 h
Result: Upregulated the proapoptotic protein Bax, downregulated the antiapoptotic protein Bcl-2, and strongly activated caspase-3 in A549 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations.
Upregulated Bax, downregulated Bcl-2, and activated caspase-3 in H446 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations, especially at 100 nM.
体内研究
(In Vivo)

MG16 (5 mg/kg；静脉注射；每隔 1 天 1 次) 可达到 75.11% 的肿瘤抑制率，在小鼠 LLC 皮下肿瘤模型中表现出强效的肺癌生长抑制作用[1]。
MG16 (5 mg/kg；静脉注射；每隔 1 天 1 次) 在小鼠 A549 皮下肿瘤模型中可实现 80.5% 的肿瘤抑制率，表现出强效的肺癌生长抑制活性[1]。

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

471.89

Formula

C23H22ClN3O6
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

MG16 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:

MG162349329-01-5MG 16MG-16Drug DerivativeApoptosisCDKASK1Drug derivativeCyclin dependent kinaseApoptosis signal-regulating kinase 1MAP3K5MAPKKK5Mitogen-activated protein kinase kinase kinase 5MEK kinase 5human lung cancer xenograft mouse modelsLewis lung carcinoma cellsmitochondrial apoptotic pathwayslung cancer cellshuman lung cancer cell linesG0/G1 cell cycle arrestcyclin-dependent kinase 6G1-to-S phase cell cycle transitionsyngeneic Lewis lung carcinoma mouse modelsapoptosis signal-regulating kinase 1Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182071
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