
PR5-LL-CM01
CAS No. 1005307-86-7
PR5-LL-CM01 ( PR5-LL-CM01 )
产品货号. M10045 CAS No. 1005307-86-7
PR5-LL-CM01 是一种新型选择性 PRMT5 甲基转移酶小分子抑制剂,IC50 为 7.5 uM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥1002 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称PR5-LL-CM01
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述PR5-LL-CM01 是一种新型选择性 PRMT5 甲基转移酶小分子抑制剂,IC50 为 7.5 uM。
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产品描述PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM; displays >10-fold selectivity over PRMT3, and no inhibitory activity over PRMT1/4/6/8; exhibits cell viability inhibition with IC50 of 2-4 uM in PDAC cells, IC50 of 10-11 uM in CRC cells, more potent than EPZ015666; significantly inhibits NF-κB activation in PDAC and CRC cells, and shows dramatic anti-tumor efficacy in vivo.
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体外实验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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体内实验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.
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同义词PR5-LL-CM01
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通路Chromatin/Epigenetic
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靶点HMTase
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受体HMTase
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研究领域——
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适应症——
化学信息
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CAS Number1005307-86-7
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分子量401.518
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分子式C23H27N7
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 11.11 mg/mL (27.67 mM)
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SMILESCC1=CC=C(NC2=C3C(N(C4=CC=CC=C4)N=C3)=NC(NCCN(C)C)=N2)C=C1C
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化学全称N6-(2-(dimethylamino)ethyl)-N4-(3,4-dimethylphenyl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Prabhu L, et al. Oncotarget. 2017 Jun 20;8(25):39963-39977.