EPZ015666 (GSK3235025)|1616391-65-1--Shanghai xingMo Biotechnology

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Description

EPZ015666, also known as GSK3235025, is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.

Chemical Structure

Chemical Name

(S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

SMILES Code

O=C(C1=NC=NC(NC2COC2)=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3

Theoretical Analysis

XingMo Cat#:XM171
Product Name:EPZ015666 (GSK3235025)
Synonyms:EPZ015666; EPZ-015666; EPZ 015666; GSK3235025; GSK-3235025; GSK 3235025.
CAS#:1616391-65-1
Chemical Formula:C₂₀H₂₅N₅O₃
Exact Mass:383.19574
Molecular Weight:383.452

Technical Data

Appearance: solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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