RRD-251

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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。

RRD-251 

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。

RRD-251

RRD-251 Chemical Structure

CAS No. : 72214-67-6

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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[1].

IC50 & Target

Rb-Raf-1 interaction, apoptosis[1]
体外研究
(In Vitro)

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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[1]

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[1]

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
(In Vivo)

RRD-251 (50 mg/kg; i.p.; q.o.d; for 14 days) has anti-cancer activities in vivo on melanomas[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-wk-old female athymic nude mice, with SK-ME-28 xenograft[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal administration, qod, for 14 days
Result: Inhibits the growth of SK-ME-28 xenograft in nude mice.

分子量

271.59

Formula

C8H9Cl3N2S
CAS 号

72214-67-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

  • [1]. Sandeep Singh, et al. Rb-Raf-1 interaction disruptor RRD-251 induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine. Mol Cancer Ther. 2010 Dec; 9(12): 3330–3341.

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