DMUP

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

DMUP 

DMUP 是一种有效的 CD47-SIRPα axis 抑制剂。DMUP 在 A549 细胞中诱导细胞凋亡 (apoptosis) 并增加巨噬细胞的吞噬作用。DMUP 降低 CD47 和 SIRPα 的蛋白表达水平。DMUP 显示出抗肿瘤活性。

DMUP

DMUP Chemical Structure

CAS No. : 2364350-07-0

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生物活性

DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity[1].

体外研究
(In Vitro)

DMUP (72 h) shows antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 µM for A549, A549/DDP, PANC-1, HepG2 cells, respectively[1].
DMUP (5 µM, 24 h) arrests the cell cycle in S phase in A549 cells[1].
DMUP (5 µM, 48 h) induces apoptosis in A549 cells[1].
DMUP (5 µM, 24 h) decreases the expression of CD47 and SIRPα protein[1].
DMUP (5 µM, 4 h) increases the macrophage phagocytosis in A549-GFP cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, A549/DDP, PANC-1, HepG2 cells
Concentration: 0-64 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 µM for A549, A549/DDP, PANC-1, HepG2 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 5 µM
Incubation Time: 24 h
Result: Arrested the cell cycle in the S phase.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 5 µM
Incubation Time: 48 h
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: A549, THP-1 cells
Concentration: 5 µM
Incubation Time: 24 h
Result: Decreased the expression of CD47 and SIRPα protein.

体内研究
(In Vivo)

DMUP (10 mg/kg, i.v., every other day for 17 day) shows antitumor activity[1].
DMUP (5, 10, 20, 40 mg/kg, i.v.,every two days for 18 days) shows no toxicity in mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice[1]
Dosage: 5, 10, 20, 40 mg/kg
Administration: i.v., every two days, 18 days
Result: Showed low toxicity with LD50 of greater than 20 mg/kg.
Animal Model: A549 xenograft BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: i.v., every other day, 17 day
Result: Showed antitumor activity.

分子量

766.44

Formula

C24H24Cl2N2O10Pt

CAS 号

2364350-07-0

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.

参考文献
  • [1]. Tan Y, et al. Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer. Eur J Med Chem. 2022; 229:114047.

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