1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. D5B

D5B 是一种有效的和选择性的 PD-L1 抑制剂。D5B 已被 DBCO 修饰。D5B 在 4T1 和 B16-F10 肿瘤细胞中降解 PD-L1EC50 分别为 5.4 μM 和 6.2 μM。D5B 可阻断 PD-L1/PD-1 相互作用,具有抗肿瘤活性。

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D5B Chemical Structure

D5B Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity[1].

IC50 & Target

EC50: 5.4 μM (PD-L1 in 4T1 tumor cells)[1]
EC50: 6.2 μM (PD-L1 in B16-F10 tumor cells)[1]

体外研究
(In Vitro)

D5B (0-10 μM;24 小时) 在 4T1 和 B16-F10 肿瘤细胞中能够降解 PD-L1,EC50 分别为 5.4 μM 和 6.2 μM[1]
D5B (0-5 μM;48 小时) 在 IFN-γ 处理和叠氮化物标记的 4T1 和 B16-F10 肿瘤细胞中,显著降低细胞膜表面 PD-L1 丰度[1]

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

Western Blot Analysis[1]

Cell Line: IFN-γ treated and azide-labeled 4T1 and B16-F10 tumor cells
Concentration: 0, 1.25, 2.5 and 5.0 μM
Incubation Time: 48 h
Result: Significantly reduced the level of PD-L1.
体内研究
(In Vivo)

D5B (5 mg/kg;静脉注射;单剂量) 在小鼠肿瘤模型中具有抗肿瘤的作用,与放疗联合效果更好。(D5B 为 PCPGd@D5B 纳米颗粒形式)[1]

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

Animal Model: 4T1 tumor-bearing mice with radiotherapy[1]
Dosage: 5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
Administration: Intraperitoneal injection (i.p.); Single dose
Result: Completely eradicated 50% of the tumor xenografts, with 60% of the tumor-bearing mice survived over 100 days.
Increased the percentage of tumor-infiltrating IFN-γ+CD8+ T cells.
Efficiently provoked an adaptive antitumor immune response for tumor regression.
Animal Model: B16-F10 tumor-bearing mice with radiotherapy[1]
Dosage: 5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
Administration: Intraperitoneal injection (i.p.); Single dose
Result: Suppressed 95% of tumor growth, with complete tumor elimination in 43% of the tumor-bearing mice and elongated survival time over 50 days.
Effectively suppressed PD-L1 expression on the surface of tumor cells and TAM membrane.
Promoted the increase of tumor infiltrating CD8+ T cells.
分子量

983.15

Formula

C58H66N2O12

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
  • 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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D5B
目录号:
HY-169392
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