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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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥1002 有现货
100MG 获取报价 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    PR5-LL-CM01
  • 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
  • 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。
  • 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.
  • 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.
  • 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.
  • 同义词
    PR5-LL-CM01
  • 通路
    Chromatin/Epigenetic
  • 靶点
    HMTase
  • 受体
    HMTase
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1005307-86-7
  • 分子量
    401.518
  • 分子式
    C23H27N7
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO : 11.11 mg/mL (27.67 mM)
  • SMILES
    CC1=CC=C(NC2=C3C(N(C4=CC=CC=C4)N=C3)=NC(NCCN(C)C)=N2)C=C1C
  • 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

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Prabhu L, et al. Oncotarget. 2017 Jun 20;8(25):39963-39977.
产品手册
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