2. PROTAC Immunology/Inflammation
  3. PROTACs PD-1/PD-L1
  4. PROTAC PD-L1 degrader-1

PROTAC PD-L1 degrader-1 是一种基于 CRBN 的 PD-L1-PROTAC 降解剂，具有显著的 PD-L1 蛋白降解能力。PROTAC PD-L1 degrader-1 在 4T1 细胞中表现出强大的 PD-L1 降解能力，DC50 为 0.609 μM。PROTAC PD-L1 degrader-1 可用于乳腺癌的研究。（蓝色：CRBN 配体 (HY-150839)，黑色：连接子；粉色：PD-L 抑制剂 (HY-19745)）。

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PROTAC PD-L1 degrader-1 Chemical Structure

PROTAC PD-L1 degrader-1 Chemical Structure

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PROTAC PD-L1 degrader-1 相关抗体

Top Publications Citing Use of Products

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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 PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745))[1].

IC50 & Target[1]

Cereblon

131.77 μM (Kd)

体外研究
(In Vitro)

PROTAC PD-L1 degrader-1（化合物 PA8；0.078-10 μM；24 小时）对 4T1 细胞中的 PD-L1 蛋白表现出显著的降解作用，且呈剂量依赖性[1]。
PROTAC PD-L1 degrader-1 与 CRBN 和 PD-L1 特异性结合，Kd 值分别为 131.77 μM 和 59.2 μM，且均呈浓度依赖性[1]。

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

PROTAC PD-L1 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: 4T1 cells
Concentration: 0.078 μM, 0.156 μM, 0.312 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Displayed a significant degradation effect on PD-L1 protein in 4T1 cells.
体内研究
(In Vivo)

PROTAC PD-L1 degrader-18（30-60 mg/kg；腹腔注射；每天一次，持续 15 天）可抑制 4T1 荷瘤小鼠模型中的肿瘤体积和肿瘤重量[1]。
PROTAC PD-L1 degrader-1 (compound PA8) 在雄性 Sprague-Dawley 大鼠中的药代动力学参数[1]。
1.19

Plasma PK properties CL (mL/min/kg) Vss (L/kg) (ng▪h/mL) Tmax (h) Cmax (ng/mL) T1/2 (h)
i.v (3 mg/kg) 471.0 23.0 / / 0.952
i.p (30 mg/kg) / / 2.0 217.0 5.3

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

Animal Model: 6-8 week old female BALB/c mice injected with 4T1 cells[1].
Dosage: 30 and 60 mg/kg
Administration: ip; once daily for 15 days
Result: The antitumor effect can be obviously observed.
分子量

777.95

Formula

C45H55N5O7
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 PD-L1 degrader-1 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 PD-L1 degrader-1PROTACsPD-1/PD-L1PD-1/Programmed death-ligand 1PD-L1-PROTAC degraderCRBNbreast cancerInhibitorinhibitorinhibit

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产品名称：
PROTAC PD-L1 degrader-1
目录号：
HY-163757
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