2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs Aurora Kinase
  4. AurAP14

AurAP14 是一种 Aurora A PROTAC 降解剂（DC50 = 120 nM）。AurAP14 对多种肿瘤细胞系显示出显著的抑制活性，在 A549 细胞中的 IC50 为 0.294 μM，在 MCF-7 细胞中为 0.534 μM。AurAP14 诱导 A549 细胞发生凋亡 (apoptosis) 并使其停滞于 S 和 G2/M 期。AurAP14 在 A549 和 A549/PTR 裸鼠异种移植模型中展示出抗肿瘤疗效。AurAP14 可用于研究 Aurora A 过表达的非小细胞肺癌 (NSCLC) 治疗。(粉色：Aurora A 配体 (HY-10971)，蓝色：E3 连接酶配体 (HY-W437598)，黑色：连接子)。

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AurAP14

AurAP14 Chemical Structure

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AurAP14 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker)[1].

IC50 & Target[1]

Aurora A

120 nM (DC50)

体外研究
(In Vitro)

AurAP14 (0.1-4 μM) 降解 Aurora A，抑制 Aurora A 介导的 p53 (Ser315) 磷酸化，并破坏 MCF-7 和 A549 细胞中原癌基因蛋白 C-MYC 的非催化保护作用[1]。
AurAP14 (0.5 μM, 24 h) 抑制 A549 细胞的迁移和菌落形成，并使 A549 细胞停滞于 S 和 G2/M 期[1]。
AurAP14 (0.5 μM, 24-48 h) 诱导 A549 细胞凋亡[1]。

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

AurAP14 相关抗体:

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Arrested A549 cells in the S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 μM
Incubation Time: 12, 24, 48 h
Result: Induced apoptosis in A549 cells.
体内研究
(In Vivo)

AurAP14 (30 mg/kg，腹腔注射， 每 2 天一次，持续 21 天) 在 A549 和 A549/PTR 裸鼠异种移植模型中实现肿瘤生长抑制[1]。

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

Animal Model: A549 cells and A549/PTR cells (1.5×107 cells/100 μL) were subcutaneously implanted into the armpits of 5-week-old male BALB/c nude mice[1]
Dosage: 30 mg/kg
Administration: i.p., once every 2 days, 21 days
Result: Achieved tumor growth inhibition (TGI) rates of 59.6% and 56.6% in A549 and A549/PTR nude mouse xenograft models, respectively.
Showed no significant changes in body weight and no obvious organ toxicity.
Reduced Aurora A expression in tumor tissues by more than 50%.
分子量

1042.98

Formula

C54H54Cl2FN11O6
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

AurAP14 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:

AurAP14AurAP 14AurAP-14PROTACsAurora KinaseAurora APROTACdegraderA549A549/PTRMCF-7 cellscancerInhibitorinhibitorinhibit

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