| 产品介绍 |
CUDC-907 is a potent inhibitor of class I PI3K kinases with an IC50 of 19 nM, 54 nM, 311 nM and 39 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ. It also potently inhibits HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 with IC50 of 1.7 nM, 5 nM, 1.8 nM, 27 nM, 2.8 nM and 5.4 nM respectively. Through its simultaneous HDAC inhibitory activity, CUDC-907 durably inhibits the PI3K-AKT-mTOR pathway and compensatory signaling molecules such as RAF, MEK, MAPK, and STAT-3, as well as upstream receptor tyrosine kinases. CUDC-907 induces apoptosis and G2–M cell-cycle arrest in cancer cells and effectively inhibits more than 50 different cancer cells鈥?growth. It may potentially evade drug resistance in cancer cells. CUDC-907 also inhibits targets and tumor growth in xenograft tumor models. Currently CUDC-907 is in phase I clinical trials for patients with solid tumors or lymphoma.
|
