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编 号:F741928
分子式:C23H27N7
分子量:401.51
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.

体内研究:
PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect.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.

体外研究:
PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 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.
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