RRD-251盐酸盐是Rb / Raf-1相互作用的可逆，有效和选择性破坏剂。视网膜母细胞瘤抑癌蛋白（Rb）通过抑制E2F转录因子家族的转录活性来控制G1-S边界。Raf-1激酶在G1期早期与Rb结合并使其磷酸化。RRD-251在体内以Rb依赖性方式显着抑制血管生成和肿瘤生长。RRD-251不会抑制B-Raf与Rb的结合以及Raf-1与Mek1 / 2的结合。同样，RRD-251不会影响与细胞周期蛋白D，细胞周期蛋白E或Raf-1相关的激酶活性。 RRD-251 hydrochloride is a reversible, potent, and selective disruptor of Rb/Raf-1 interaction. The retinoblastoma tumor suppressor protein (Rb) controls the G1-S boundary by repressing the transcriptional activity of the E2F family of transcription factors. Raf-1 kinase binds and phosphorylates Rb early in the G1 phase. RRD-251 significantly inhibits angiogenesis and tumor growth in vivo in an Rb-dependent manner. RRD-251 does not inhibit the binding of B-Raf to Rb and Raf-1 to Mek1/2. Also, RRD-251 does not affect the kinase activities associated with cyclin D, cyclin E, or Raf-1.