2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs Anaplastic lymphoma kinase (ALK) Apoptosis
  4. ALK degrader 2

ALK degrader 2 是一种具有口服活性的 ALK 降解剂，降解 EML4-ALK 蛋白水平 (DC50 = 8 nM) 和核磷蛋白 (NPM)-ALK 蛋白水平 (DC50 = 102 nM)。ALK degrader 2 通过 Hsp70 伴侣系统和泛素-蛋白酶体途径介导 ALK 降解。ALK degrader 2 在 H3122 细胞中诱导显著的 S 期细胞周期阻滞和细胞凋亡 (apoptosis)。ALK degrader 2 在 H3122 异种移植瘤的小鼠中显示出抗肿瘤活性。ALK degrader 2 可用于非小细胞肺癌 (NSCLC) 的研究。(粉色: ALK 配体 (HY-W754809), 蓝色: Hyt 配体 (HY-W013021), 黑色: 连接子 (HY-Y1760), ALK 配体-连接子偶联物 (HY-175528))。

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

ALK degrader 2

ALK degrader 2 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

ALK degrader 2 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528))[1].

体外研究
(In Vitro)

ALK degrader 2 (Compound J26) (72 h) 在 H3122 细胞中显示出抗增殖作用 (IC50 = 25 nM)[1]。
ALK degrader 2 (0.015-5 μM, 24 h) 在 H3122 细胞中降解 EML4-ALK 水平 (DC50 = 8 nM)，在 SU-DHL-1 细胞中降解核磷蛋白 (NPM)-ALK 蛋白水平 (DC50 = 102 nM)[1]。
ALK degrader 2 (0.01-0.5 μM, 24 h) 在 H3122 细胞中诱导显著的 S 期细胞周期阻滞和细胞凋亡[1]。
ALK degrader 2 (0.5 μM, 24 h) 通过 Hsp70 伴侣和泛素-蛋白酶体途径介导 ALK 降解，不涉及 E3 连接酶 (CRBN, TTC3, ARK2N)[1]。

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

ALK degrader 2 相关抗体:

Apoptosis Analysis[1]

Cell Line: H3122 cells
Concentration: 0.01, 0.05, 0.5 μM
Incubation Time: 24 h
Result: Induced apoptosis in H3122 cells.

Cell Cycle Analysis[1]

Cell Line: H3122 cells
Concentration: 0.01, 0.05, 0.5 μM
Incubation Time: 24 h
Result: Induced significant S-phase cell cycle arrest in H3122 cells.
体内研究
(In Vivo)

ALK degrader 2 (Compound J26) (10 mg/kg，静脉给药，单次给药) 在 H3122 异种移植瘤的雌性 BALB/c 裸鼠中，于给药后 24 小时显著降低肿瘤组织中的 EML4-ALK 蛋白水平，并持续抑制至 72 小时[1]。
ALK degrader 2 (20 mg/kg，口服给药 或 5-10 mg/kg，静脉给药，每隔一天给药一次，持续 21 天) 在 H3122 异种移植瘤的小鼠中显示出抗肿瘤活性[1]。

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

Animal Model: H3122 cells (1 × 106 in appropriate volume) were subcutaneously implanted into the right flanks of 4-week-old female BALB/c nude mice to establish H3122 xenograft tumor models[1]
Dosage: 20 mg/kg (p.o.) or 5, 10 mg/kg (i.v.)
Administration: once every other day for 21 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight and no other signs of toxicity.
Significantly reduced EML4-ALK and phosphorylated ALK (p-ALK) protein levels in tumor tissues.
Induced significant tumor cell apoptosis.
分子量

644.85

Formula

C40H48N6O2
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

ALK degrader 2 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:

ALK degrader 2ALK degrader2ALK degrader-2PROTACsAnaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246non-small cell lung cancer (NSCLC)ALKPROTACH3122 cellsInhibitorinhibitorinhibit

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：
ALK degrader 2
目录号：
HY-175527
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