SKLB-163

SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis^[1][2]. In Vitro:SKLB-163 (0-20 μM, 48 h) inhibits proliferation and migration of nasopharyngeal carcinoma (NPC) cells, and sensitizes cells to irradiation^[1].
SKLB-163 (0-20 μM, 48 h) shows cytotoxicity effect in A375, SPC-A1, SW620, HeLa, PC-3 cells^[2].
SKLB-163 (0-2.5 μM, 48 h) induces A375 cell apoptosis and inhibits colony information^[2].
In Vivo:SKLB-163 (25-100 mg/kg, i.g., once daily for 30 days) inhibits tumor growth and ascites formation, and inhibits liver and lung metastasis in NPC lung metastatic mice model^[1].
SKLB-163 (50 mg/kg, once daily. from the 6th day of SKLB-163 administration, 3 Gy radiation once per day for 3 days) sensitizes NPC tumor to irradiation in CNE-2 and C666-1 subcutaneous xenograft mice models^[1].