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  3. PROTAC BRD4 Degrader-45

PROTAC BRD4 Degrader-45 (compound 2b) 是一种靶向 BRD4 的 PROTAC降解剂。PROTAC BRD4 Degrader-45 表现出增强的被动膜通透性、在添加 10% FBS 的细胞培养基中的稳定性,以及在癌细胞中更高的细胞内浓度。

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PROTAC BRD4 Degrader-45

PROTAC BRD4 Degrader-45 Chemical Structure

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Customer Review

Other Forms of PROTAC BRD4 Degrader-45:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells[1].

体外研究
(In Vitro)

PROTAC BRD4 Degrader-45 (compound 2b) (10-10000 nM; 4 h) 可在 MCF-7 细胞中诱导 BRD4 降解,其 DC50 为 43 nM[1]
PROTAC BRD4 Degrader-45 (compound 2b) (10 μM; 4 h at 37 °C) 在 PAMPA 试验中的 Papp 值为 1.20,显示出中等水平的被动膜通透性[1]
PROTAC BRD4 Degrader-45 (compound 2b) (1 μM; 30 min at 37 °C (liver microsome assay); 6 h at 37 °C (media stability assay)) 在含 10% FBS 的细胞培养基中孵育 6 h 后稳定性>90%,在无 NADPH 的小鼠肝微粒体中稳定性也>90%,但在含 NADPH 的微粒体中会发生显著代谢,仅剩余 1.08%[1]
PROTAC BRD4 Degrader-45 (compound 2b) (10 μM; 0 h, 30 min, 6 h) 在 MCF-7 细胞中表现出更优异的膜吸附能力,且在处理后 30 min 时达到最高细胞内浓度[1]

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

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10-10000 nM
Incubation Time: 4 h
Result: Induced BRD4 degradation with a half-maximal degradation concentration (DC50) of 43 nM.
Showed a hook effect.
分子量

800.28

Formula

C39H38ClN7O8S

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 BRD4 Degrader-45 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.

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产品名称:
PROTAC BRD4 Degrader-45
目录号:
HY-181553A
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