2. Protein Tyrosine Kinase/RTK PROTAC Apoptosis
  3. Bcr-Abl PROTACs Apoptosis
  4. PROTAC BCR-ABL Degrader-2

PROTAC BCR-ABL Degrader-2 是一种选择性的 Bcr-AblT315 PROTAC 降解剂，在 Ba/F3 Bcr-AblT315I 细胞中的 DC50 为 108.7 nM。PROTAC BCR-ABL Degrader-2 展现出强效的降解能力，在 100 nM 和 300 nM 浓度下，降解率分别达到 69.89% 和 94.23%。PROTAC BCR-ABL Degrader-2 在体内表现出良好的血浆暴露量，能诱导显著的肿瘤消退诱导癌细胞凋亡 (apoptosis)，且安全性良好。PROTAC BCR-ABL Degrader-2 可用于慢性髓系白血病的研究。
(粉色: Bcr-Abl 配体 (HY-15666)；蓝色: Cereblon 配体 (HY-10984)；黑色: 连接子)。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

PROTAC BCR-ABL Degrader-2

PROTAC BCR-ABL Degrader-2 Chemical Structure

CAS No. : 2703834-25-5

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 BCR-ABL Degrader-2 相关抗体

Top Publications Citing Use of Products

查看 Bcr-Abl 亚型特异性产品:

查看所有亚型
Abl Bcr-Abl

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

PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research[1][2]. (Pink: Bcr-Abl ligand (HY-15666); Blue: Cereblon ligand (HY-10984); Black: linker).

体外研究
(In Vitro)

PROTAC BCR-ABL Degrader-2 (Compound 7o) 针对 K562 及 Ba/F3 Bcr-AblWT 细胞的IC50 分别为 7.7 nM 与 4.2 nM[1]。
PROTAC BCR-ABL Degrader-2 (0-300 nM) 在 Ba/F3 Bcr-AblT315I 细胞中可显著降低 Bcr-AblT315I 蛋白水平，DC50 为108.7 nM[1]。
PROTAC BCR-ABL Degrader-2 (0-300 nM，0-48 小时) 在 Bcr-AbllT315I 细胞中通过 CRBN E3泛素化途径诱导 Bcr-AblT315I 蛋白降解，并呈现"钩状效应" [1]。

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

PROTAC BCR-ABL Degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: Ba/F3 Bcr-AblT315I and K562 cells
Concentration: 100 nM
Incubation Time: 0, 1, 2, 4, 6, 8, 10, 12, 24, 36 and 48 h
Result: Caused the degradation of Bcr-AblT315I protein in a time-dependent manner.
Reduced Bcr-AblT315I protein level substantially after 6h treatment while appeared a “hook” effect during 8-10h treatment.
Observed the maximum degradation after24h treatment.
Displayed a different trend for reducing Bcr-AblWT in K562cells with substantially reduction after 36h treatment (this different might be associated with the different states of E3 ligase in Ba/F3Bcr-AblT315I and K562 cells.).

Immunofluorescence[1]

Cell Line: MG132 (HY-13259) (20 ) Ba/F3 Bcr-AblT315I cells
Concentration: 100 and 300 nM
Incubation Time: 24 h
Result: Induced Bcr-AblT315I degradation rescuing by MG132.
体内研究
(In Vivo)

PROTAC BCR-ABL Degrader-2 (compound 7o) (20 mg/kg，单次腹腔注射) 在 ICR 小鼠中血浆浓度在 48 小时内维持较高水平[1]。
PROTAC BCR-ABL Degrader-2 (10-20 mg/kg，腹腔注射，每两日一次、持续 14 天) 在 Ba/F3 Bcr-AblT315I 异种移植瘤小鼠模型中，展现出显著的抗肿瘤活性与良好的安全性[1]。

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

Animal Model: Ba/F3 cells expressing Bcr-AblT315I (2 x 106 cells/0.1 mL) induced-CB17-SCID mice [1]
Dosage: 10 or 20 mg/kg
Administration: i.p., once every two days for 14 days
Result: Obviously sup pressed the growth of Ba/F3 Bcr-AblT315I xenograft tumor with a tumor growth inhibition (TGI) value of 90.8% at the dose of 20 mg/kg.
Induced the Bcr-AblT315I degradation and apoptosis.
Resulted no mortality or significant body weight loss.
分子量

901.93

Formula

C48H46F3N9O6
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

PROTAC BCR-ABL 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:

PROTAC BCR-ABL Degrader-22703834-25-5Bcr-AblPROTACsApoptosisBa/F3 Bcr-AblT315I cellshigh plasma exposurechronic myeloid leukemiaInhibitorinhibitorinhibit

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 BCR-ABL Degrader-2
目录号：
HY-180967
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