| Bioactivity | 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]. |
| Target | Rb-Raf-1 interaction, apoptosis |
| Invitro | 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: |
| 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: |
| Name | RRD-251 |
| CAS | 72214-67-6 |
| Formula | C8H9Cl3N2S |
| Molar Mass | 271.59 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |