1. Apoptosis
  2. Apoptosis
  3. TREM2-IN-1

TREM2-IN-1 (OPA) 是来自奥沙利铂和青蒿琥酯的 TREM2 抑制剂。TREM2-IN-1 可以缓解免疫抑制的肿瘤微环境,增强化学抗癌效果。TREM2-IN-1 通过减少 CD206+ 和 CX3CR1+ 免疫抑制性巨噬细胞的数量来抑制小鼠模型中携带 MC38 结直肠肿瘤的肿瘤生长。TREM2-IN-1 还促进免疫刺激性树突细胞、细胞毒性 T 细胞和自然杀伤细胞的扩展和浸润。

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TREM2-IN-1

TREM2-IN-1 Chemical Structure

CAS No. : 2000236-36-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206+ and CX3CR1+ immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells[1].

IC50 & Target

TREM2[1]

体外研究
(In Vitro)

TREM2-IN-1 (0.8 μM, 72 h) 在 HCT-116 细胞中抑制 DNA 合成的前期 (G1 期),并具有强大的促凋亡能力[1]
TREM2-IN-1 (1 μM, 24 h) 显著抑制了 THP-1 衍生巨噬细胞中 TREM2 的表达[1].

TREM2-IN-1 在 72 小时内对不同细胞系的 IC50 (μM)[1]

Complex HCT-116 HepG2 PANC-1 U87-MG HK-2
TREM2-IN-1 0.84 7.32 5.26 22.23 16.29

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

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.8 μM
Incubation Time: 72 h
Result: Increased the cells in the G1 phase from 24.81% to 48.96% in HCT-116 cells.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.8 μM
Incubation Time: 72 h
Result: Induced 5.17% and 30.9% of HCT-116 cells to enter the early and late apoptosis respectively at 0.8 μM.
体内研究
(In Vivo)

TREM2-IN-1 (1.5 mg Pt per kg, 治疗,单次剂量, 持续 15 天) 在携带 MC38 小鼠结肠癌的 C57BL/6 小鼠模型中,能够有效抑制肿瘤生长,并且整体毒性较低[1]

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

Animal Model: C57BL/6 mice models bearing MC38 murine colorectal cancer[2]
Dosage: 1.5 mg Pt per kg
Administration: treat, a single dose for 15 days
Result: Effectively suppressed the tumor growth to the volume of 185.75 mm3 in C57BL/6 mice models bearing MC38 murine colorectal cancer.
分子量

1164.12

Formula

C46H68N2O20Pt

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献
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  • 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:
TREM2-IN-1
目录号:
HY-160421
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