| 产品描述: | PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies |
| 靶点: |
PRMT5 |
| 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. |
| 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. |
| 参考文献: |
1. Prabhu L, et al. Adapting AlphaLISA high throughput screen to discover a novel small-molecule inhibitor targeting protein arginine methyltransferase 5 in pancreatic and colorectal cancers. Oncotarget. 2017;8(25):39963-39977. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 备注: |
PR5-LL-CM01 是一种有效的 (PRMT5) 抑制剂 (IC50= 7.5 μM)。PR5-LL-CM01 具有抗肿瘤活性。 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.491 ml |
12.453 ml |
24.906 ml |
| 5 mM |
0.498 ml |
2.491 ml |
4.981 ml |
| 10 mM |
0.249 ml |
1.245 ml |
2.491 ml |
| 50 mM |
0.05 ml |
0.249 ml |
0.498 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |