PR5-LL-CM01

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor ( IC 50 = 7.5 μM). Anti-tumor activies. In Vitro PR5-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 Vivo PR5-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

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet