PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.

Product information

CAS Number: 1005307-86-7

Molecular Weight: 401.51

Formula: C23H27N7

Chemical Name: N6-[2-(dimethylamino)ethyl]-N4-(3, 4-dimethylphenyl)-1-phenyl-1H-pyrazolo[3, 4-d]pyrimidine-4, 6-diamine

Smiles: CN(C)CCNC1N=C(NC2C=CC(C)=C(C)C=2)C2C=NN(C3C=CC=CC=3)C=2N=1

InChiKey: UPAZOMJFUXPAJI-UHFFFAOYSA-N

InChi: InChI=1S/C23H27N7/c1-16-10-11-18(14-17(16)2)26-21-20-15-25-30(19-8-6-5-7-9-19)22(20)28-23(27-21)24-12-13-29(3)4/h5-11,14-15H,12-13H2,1-4H3,(H2,24,26,27,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

In Vivo:

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

References:

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.

Products are for research use only. Not for human use.