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.