EPZ015666 | Potent and selective PRMT5 inhibitor

CAS:
1616391-65-1
Catalog Number:
10-4031
Activity:
Potent and selective PRMT5 inhibitor
Chemical Name:
(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Molecular Weight:
383.44
Molecular Formula:
C20H25N5O3
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$90.00
25 mg$325.00

EPZ015666 (1616391-65-1) is a selective and potent (IC50 = 22nM) inhibitor of arginine methyltransferase 5 (PRMT5).1,2 PRMT5 inhibition with EPZ015666 potently suppressed in vivo glioblastoma tumors3 and significantly inhibited the growth of multiple myeloma cell lines4.

References/Citations:

1) Chan-Penebre et al. (2015), A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models; Nat. Chem. Biol. 11 432
2) Duncan et al. (2015), Structure and Property Guided Design in the Identification of PRMT5 Toll Compound EPZ015666; ACS Med. Chem. Lett. 7 162
3) Braun et al. (2017), Coordinated Splicing of Regulatory Detained Introns within Oncogenic Transcripts Creates an Exploitable Vulnerability in Malignant Glioma; Cancer Cell 32 411
4) Gulia et al. (2018), Protein arginine methyltransferase 5 has prognostic relevance and is a druggable target in multiple myeloma; Leukemia 32 996

CAS:
1616391-65-1
Catalog Number:
10-4031
Activity:
Potent and selective PRMT5 inhibitor
Chemical Name:
(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Molecular Weight:
383.44
Molecular Formula:
C20H25N5O3
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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