RRD-251
目录号 : KM10185 CAS No. : 72214-67-6 纯度 : 98%

RRD-251 是一种视网膜母细胞瘤肿瘤抑制蛋白 (Rb)-Raf-1相互作用 (Rb-Raf-1 interaction) 的抑制剂,具有高效的抗增殖、抗血管生成和抗肿瘤活性。

规格 价格 是否有货 数量
5mg
In-stock

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生物活性

RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.

体外研究

RRD-251 (10-50 μM; 24 hours) inhibits melanoma growth in-vitro.
RRD-251 (50 μM; 2 hours) inhibits Rb-Raf-1 interaction and Rb phosphorylation in non-small cell lung cancer cells.
RRD-251 induces apoptosis (50 μM; 18 hours) and cell cycle arrest (20-50 μM; 4 hours).
RRD-251 alters the expression of cell cycle and apoptosis regulatory protein.

Cell Proliferation Assay

Cell Line: SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells
Concentration: 10 μM, 20 μM, 50 μM
Incubation Time: 24 hours
Result: Inhibited melanoma growth in-vitro.

Western Blot Analysis

Cell Line: SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells
Concentration: 50 μM
Incubation Time: 2 hours
Result: Showed the depletion of phosphorylated-Rb in RRD-251 treated cells.

Apoptosis Analysis

Cell Line: SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells
Concentration: 50 μM
Incubation Time: 18 hours
Result: Induced apoptosis.

Cell Cycle Analysis

Cell Line: SK-MEL-28 cells , SK-MEL-5 cells
Concentration: 20 μM, 50 μM
Incubation Time: 4 hours
Result: Resulted in a dose dependent inhibition of cell cycle progression in SK-MEL-28 and SK-MEL-5 cells, respectively.
体内研究

RRD-251 (50 mg/kg; i.p.; q.o.d; for 14 days) has anti-cancer activities in vivo on melanomas.

Animal Model: 8-wk-old female athymic nude mice, with SK-ME-28 xenograft
Dosage: 50 mg/kg
Administration: Intraperitoneal administration, qod, for 14 days
Result: Inhibits the growth of SK-ME-28 xenograft in nude mice.
分子式
C8H9Cl3N2S
分子量
271.59
CAS号
72214-67-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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