| Identification | Back Directory | [Name]
1H-Pyrazolo[3,4-d]pyrimidine-4,6-diamine, N6-[2-(dimethylamino)ethyl]-N4-(3,4-dimethylphenyl)-1-phenyl- | [CAS]
1005307-86-7 | [Synonyms]
PR5 LL CM01,PR5LLCM01,PR-5-LL-CM01
1H-Pyrazolo[3,4-d]pyrimidine-4,6-diamine, N6-[2-(dimethylamino)ethyl]-N4-(3,4-dimethylphenyl)-1-phenyl- | [Molecular Formula]
C23H27N7 | [MOL File]
1005307-86-7.mol | [Molecular Weight]
401.51 |
| Chemical Properties | Back Directory | [Boiling point ]
568.2±60.0 °C(Predicted) | [density ]
1.21±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 11.11 mg/mL (27.67 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C) | [form ]
Solid | [pka]
9.01±0.28(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1]. | [in vivo]
PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1]. | 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.
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| [IC 50]
PRMT5 | [storage]
4°C, protect from light | [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. DOI:10.18632/oncotarget.18102 |
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