2. PROTAC Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs Btk Syk MEK ERK
  4. UBX-382

UBX-382 是一种具有口服活性的 BTK PROTAC 降解剂，DC50 为 4.56 nM。UBX-382 通过靶向 BTK 抑制 B 细胞受体信号传导。UBX-382 对野生型和突变型 BTK 蛋白显示出优越的降解活性。UBX-382 抑制携带野生型或 C481S 突变 BTK 的 TMD-8 细胞的小鼠异种移植模型中的肿瘤生长。UBX-382 可用于 B 细胞相关血液癌症研究。

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

UBX-382

UBX-382 Chemical Structure

CAS No. : 2884554-45-2

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 价格 是否有货 数量
1 mg ￥2400
In-stock
5 mg ￥6000
In-stock
10 mg 现货 询价
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

UBX-382 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 MEK 亚型特异性产品:

查看所有亚型
MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

UBX-382 (0.00001-10 nM，0.5-48 小时) 在 TMD-8 细胞中诱导强效的 BTK 降解，DC50 为 4.56 nM[1]。
UBX-382 (0.0001-10 μM，3-5 天) 抑制 TMD8 (IC50 = 14 nM)、WSU-DLCL2 (IC50 = 18 nM)、OCI-Ly3 (IC50 = 199 nM) 和 U2932 (IC50 = 21 nM) 的增殖，通过 Cell Titer-Glo 实验重复测定[1]。
UBX-382 (10 nM，24 小时) 显著抑制 TMD-8 细胞中 BCR 信号激活诱导的 CCL3 和 CCL4 分泌[1]。
UBX-382 (100 nM，6-24 小时) 抑制 U2932 细胞中 BTK Y223、SYK、MEK 和 ERK 的磷酸化[1]。
UBX-382 (0.1-10 μM，24 小时) 在 HEK293 细胞中有效降解野生型及多种 BTK 突变体 (E41K、C481S/R/T/Y/F、L528W)，并强烈抑制它们的磷酸化[1]。

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

UBX-382 相关抗体:

Western Blot Analysis[1]

Cell Line: U2932 cells
Concentration: 100 nM
Incubation Time: 6, 24 h
Result: Showed far more effective inhibition of BTK Y223 phosphorylation than Ibrutinib (HY-10997), Acalabrutinib (HY-17600), and Nemtabrutinib (ARQ-531) (HY-112215) in U2932 cells.
Inhibited the phosphorylation of SYK, MEK, and ERK.
体内研究
(In Vivo)

UBX-382 (3-30 mg/kg，口服，每日一次，21 天) 抑制 TMD-8 异种移植模型和 TMD-8 BTK C481S 异种移植模型中肿瘤的生长[1]。

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

Animal Model: TMD-8 cells (1 × 107 in Matrigel) were subcutaneously injected into the flanks of 6-week-old CB17/severe combined immunodeficient mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o. once daily for 21 days
Result: Achieved complete tumor regression in TMD-8 xenograft models.
Showed no significant changes in body weight and no other clinical toxicity signs during the experiment.
Reduced BTK levels in tumors of TMD-8 xenograft models.
Animal Model: TMD-8 BTK C481S cells were subcutaneously inoculated into the right flank of male CB17/severe combined immunodeficient mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o. once daily for 21 days
Result: Induced remarkable dose-dependent tumor regression in TMD-8 BTK C481S xenograft models, while Ibrutinib failed to inhibit tumor growth.
分子量

752.86

Formula

C42H44N10O4
CAS 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

UBX-382 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:

UBX-3822884554-45-2UBX382UBX 382PROTACsBtkSykMEKERKBruton tyrosine kinaseSpleen tyrosine kinaseMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesB-cell lymphomasTMD-8in murine xenograft models of TMD-8 cellsB-cell receptorBTKSYKERK,Inhibitorinhibitorinhibit

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：
UBX-382
目录号：
HY-160142
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