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. |
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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. |
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| 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 | 1 mM | 3.6820 mL | 18.4101 mL | 36.8202 mL | | 5 mM | 0.7364 mL | 3.6820 mL | 7.3640 mL | | 10 mM | 0.3682 mL | 1.8410 mL | 3.6820 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。 |
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