PR5-LL-CM01

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PR5-LL-CM01 

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。

PR5-LL-CM01

PR5-LL-CM01 Chemical Structure

CAS No. : 1005307-86-7

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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[1].

体外研究
(In Vitro)

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[1].
PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].
PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1].

Shanghai Jinpan Biotech Co Ltd 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)[1]
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.

分子量

401.51

Formula

C23H27N7
CAS 号

1005307-86-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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