RGB-286638 as a radiation sensitizer

对许多癌细胞系的实验表明，RGB-286638在所有测试的细胞系中是一种有效的辐射敏化剂，包括乳腺癌细胞系、前列腺癌细胞系、神经母细胞瘤细胞系和肺癌细胞系。 在多个细胞系中观察到有效的辐射致敏作用，其中当将该化合物加入细胞中时，实现了近50%的辐射剂量增强。 我们已经证明，这些影响与处理的细胞中双链DNA断裂的存在增加以及这些断裂的修复较慢相关。 关于死亡机制的实验表明，细胞死亡主要是由于有丝分裂灾难，这是辐射诱导细胞死亡的典型情况。 还在小鼠异种移植肿瘤模型中测试了RGB-286638与辐射的作用。我们已经开始准备发表这些结果。这种化合物在人类中有很大的应用前景。

Experiments with a number of carcinoma cell lines have shown that RGB-286638 is a potent radiation sensitizer in all cell lines tested, including breast cancer cell lines, prostate cancer cell lines, neuroblastoma cell lines, and lung cancer cell lines. Potent radiation sensitization was seen in multiple cell lines, where a nearly 50% enhancement of radiation dose was achieved when the compound was added to cells. We have demonstrated that these effects correlate with increased presence of double stranded DNA breaks in treated cells, and with slower repair of these breaks. Experiments on the mechanism of death suggest that cells die predominantly by mitotic catastrophe, as is typical for radiation-induced cell death. The effects of RGB-286638 with radiation are also being tested in a mouse xenograft tumor model. We have begun preparing these results for publication.This compound holds great promise for use in humans.