PR5-LL-CM01 is a potent PRMT5 inhibitor with an IC50 value of 7.5 μM. PR5-LL-CM01 inhibits the proliferation of PDAC cells (PANC1, MiaPaCa2, and AsPC1) with an IC50 value ranging in 2-4 μM. PR5-LL-CM01 inhibits the proliferation of CRC cells (HT29, HCT116, and DLD1) with an IC50 value of 10-11 μM. The IC50 range of PR5-LL-CM01 for CRC cells (HT29, HCT116 and DLD1) is 10-11 μM. PR5-LL-CM01 has higher specific inhibitory efficacy against cancer cells and lower toxicity to normal cells. PR5-LL-CM01 can strongly inhibit the colony forming ability of PANC1 and HT29 cells. PR5-LL-CM01 inhibits the activation of NF-κB and the expression of its target genes in PDAC and CRC cells. At a concentration of less than 15 μM, PR5-LL-CM01 significantly reduced the expression of TNFα and IL8 in PANC1 and HT29 cells[1].
PR5-LL-CM01 动物研究
Animal study
At a dose of 20 mg/kg, injected intraperitoneally 3 times per week, PR5-LL-CM01 showed significant anti-tumour effects in PANC1 and HT29 xenograft mice[1].
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