Description
PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor ( IC 50 = 7.5 µM). Anti-tumor activies.In VitroPR5-LL-CM01 has a range of IC 50 at 2-4 µM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC 50 at 10-11 µM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells. PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells. PR5-LL-CM01 (0-15 µM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells) Dosage: 20 mg/kg (drug stock dissolved in 1:1 Cremophor:ethanol solution) Administration: Intraperitoneally 3 times per week; 32 days (PANC1 model); 10 days (HT29 model) Result: Led to significant tumor inhibition in both PANC1 and HT29 xenografted mice. Did not visibly affect the mice body weight.Form:Solid