2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs EGFR Apoptosis
  4. PROTAC EGFR degrader 14

PROTAC EGFR degrader 14 是一种强效且具有选择性的 EGFR PROTAC 降解剂，其对 EGFRL858R/T790M/C797S 的DC50 值约为 2.9 nM， Dmax 为 93.1%。PROTAC EGFR degrader 14 通过 VHL 和蛋白酶体依赖性方式选择性诱导 EGFRC797S 的降解，并下调与 EGFR 相关的转录组，并对 EGFRWT 具有很高的选择性。PROTAC EGFR degrader 14 诱导细胞周期停滞和凋亡 (apoptosis)，并显著抑制肿瘤生长。PROTAC EGFR degrader 14 可用于非小细胞肺癌 (NSCLC) 的研究 (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688))。

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

PROTAC EGFR degrader 14

PROTAC EGFR degrader 14 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

PROTAC EGFR degrader 14 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 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688))[1].

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

PROTAC EGFR degrader 14 (Compound 9ea) (0-20 μM, 0-24 h) 在 PC9 (EGFRL858R/T790M/C797S) 和 PC9 (EGFRDel19/T790M/C797S) 细胞中呈浓度和剂量依赖性地降解EGFR，DC50值分别为2.9 nM 和 21.6 nM，且在 EGFR 野生型细胞系(A549，DC50 = 2157 nM) 中无活性[1]。
PROTAC EGFR degrader 14 (0.1-5 μM, 24-48 h) 在 PC9 (EGFRL858R/T790M/C797S) 和 PC9 (EGFRDel19/T790M/C797S) 细胞中诱导 G1 期阻滞和细胞凋亡[1]。
PROTAC EGFR degrader 14 (0.01-0.25 μM, 24 h) 在 PC9 (EGFRL858R/T790M/C797S) 和 PC9 (EGFRDel19/T790M/C797S) 细胞中有效减少 EGFR 降解，且这依赖于蛋白酶体和 VHL 系统[1]。

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

PROTAC EGFR degrader 14 相关抗体:

Cell Cycle Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.1, 0.5, 1 and 5 μM
Incubation Time: 24 h
Result: Increased the percentages of cells in the G1/G0 phase concentration-dependently.
Reduced the S phase populations 24.8% to 10.4% in PC9 (EGFRL858R/T790M/C797S) cells and 22.3% to 10.9% in PC9 (EGFRDel19/T790M/C797S) cells.

Apoptosis Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.1, 0.5, 1 and 5 μM
Incubation Time: 48 h
Result: Significantly promoted cell apoptosis in a concentration-dependent manner.
Reached the apoptotic rates of 22.0% and 36.5%, respectively.

Western Blot Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.01, 0.05, 0.25 μM
Incubation Time: 24 h
Result: Effectively inhibited downstream signaling proteins as the phosphorylation of STAT3, AKT and ERK1/2.
Showed weaker inhibition of EGFR and downstream signaling proteins in A549 cells.

Western Blot Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S), PC9 (EGFRDel19/T790M/C797S) cells and A549 (EGFRWT)
Concentration: 0.25 μM pretreated with MG132 (HY-13259) (10 μM), MLN4924 (HY-70062) (10 μM), and VHL ligand (10 μM and 20 μM) for 4 h
Incubation Time: 24 h
Result: Effectively blocked EGFR degradation by pretreatment with the proteasome inhibitor MG132 or the E1 neddylation inhibitor MLN4924.
Exhibited no effect in inducing EGFR degradation without VHL ligand.
体内研究
(In Vivo)

PROTAC EGFR degrader 14 (Compound 9ea) (25-50 mg/kg, i.v., 每隔一天一次, 共 15 天) 在 PC9 (EGFRL858R/T790M/C797S) 异种移植小鼠模型中能显著抑制肿瘤生长，具有强大的 EGFR 降解效果且无毒性迹象[1]。

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

Animal Model: PC9 (EGFRL858R/T790M/C797S) xenografts model in male BALB/c nude mice[1]
Dosage: 25 and 50 mg/kg
Administration: Intravenous injection (i.v.), every other day, for 15 days
Result: Demonstrated superior efficacy with the tumor growth inhibition (TGI) rate of 74.7%.
No statistically significant body weight loss was observed in mice during the treatment period.
Significantly reduced the average tumor weight.
Displayed no toxicity on the primary organs, including the heart, liver, spleen, lungs, kidneys, and brain.
Caused no significant changes in blood parameters analysis and blood biochemistry profiling.
分子量

1008.33

Formula

C57H73N11O4S
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

PROTAC EGFR degrader 14 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:

PROTAC EGFR degrader 14PROTAC EGFR degrader14PROTAC EGFR degrader-14PROTACsEGFRApoptosisEpidermal growth factor receptorErbB-1HER1nonsmall cell lung cancerPROTACXenograft mouse modelInhibitorinhibitorinhibit

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：
PROTAC EGFR degrader 14
目录号：
HY-175252
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