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RRD-251
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RRD-251图片
CAS NO:72214-67-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

RRD-251 is an inhibitor ofretinoblastoma 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].

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].

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

性状

Solid

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)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL(460.25 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.6820 mL18.4101 mL36.8202 mL
5 mM0.7364 mL3.6820 mL7.3640 mL
10 mM0.3682 mL1.8410 mL3.6820 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。