生物活性 体外研究 体内研究
ChemicalBook  CAS数据库列表  2426685-25-6

2426685-25-6

2426685-25-6,2426685-25-6,结构式
2426685-25-6
  • CAS号:2426685-25-6
  • 英文名:L-Lysine, L-serylglycyl-L-glutaminyl-L-tyrosyl-L-alanyl-L-seryl-L-tyrosyl-L-histidyl-L-cysteinyl-L-tryptophyl-L-cysteinyl-L-tryptophyl-L-arginyl-L-α-aspartyl-L-prolylglycyl-L-arginyl-L-serylglycylglycyl-L-seryl-
  • 中文名:2426685-25-6
  • CBNumber:CB58378302
  • 分子式:C107H150N34O32S2
  • 分子量:2488.7
  • MOL File:2426685-25-6.mol
2426685-25-6化学性质
  • 密度 :1.60±0.1 g/cm3(Predicted)
  • 储存条件 :Store at -20°C
  • 形态 :Solid
  • 颜色 :White to off-white

2426685-25-6性质、用途与生产工艺

  • 生物活性 TPP-1 是 PD-1/PD-L1 相互作用的有效抑制剂。TPP-1 与 PD-L1 特异性高亲和力结合 (KD=95 nM)。动物模型中,TPP-1 通过再激活 T 细胞功能抑制肿瘤生长。
  • 体外研究

    TPP-1 binds to PD-L1 with high affinity and blocks PD-1/PD-L1 interaction. The K D value of PD-L1 with TPP-1 peptide is about 95 nmol/L (around five times less than that with PD-1), The binding site of TPP-1 to PD-L1 is close to the interactive site of PD-1 and PD-L1.TPP-1 (4 μM) reactivates T-cell functions, it induces IFNγ release significantly higher than control and SPP-1, and the TPP-1 group shows similar outcomes for cell proliferation.

  • 体内研究

    TPP-1 (subcutaneous injection; 4 mg/kg; every other day eight times; 32 days) inhibits tumor growth (compared with SPP-1 and control). The growth rate in TPP-1-treated mice is 56%. And when administered in the absence of T cells (control group), TPP-1 has no effect on the growth of the H460-luc tumors.

    Animal Model: 5 to 6-week-old female Balb/c nude mice  injected with H460 cells transfected with the plvx-puro/luciferase lentiviral vector
    Dosage: 4 mg/kg
    Administration: Subcutaneous injection; 4 mg/kg; every other day eight times; 32days
    Result: Inhibited the tumor growth in a tumor xenograft model via reactivating T-cell function.
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