1. PROTAC Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt
  2. PROTACs Btk Syk MEK ERK
  3. 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

查看 PROTACs 亚型特异性产品:

查看 MEK 亚型特异性产品:

查看 ERK 亚型特异性产品:

  • 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.

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
  • 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.

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: