EPZ015666 (GSK3235025)
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MedKoo CAT#: 407226

CAS#: 1616391-65-1

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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 650 Same day
200mg USD 1050 Same day
500mg USD 2150 Same day
1g USD 3250 2 weeks
2g USD 4650 2 weeks
5g USD 8450 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-23. Prices are subject to change without notice.

EPZ015666, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407226
Name: EPZ015666 (GSK3235025)
CAS#: 1616391-65-1
Chemical Formula: C20H25N5O3
Exact Mass: 383.19574
Molecular Weight: 383.452
Elemental Analysis: C, 62.65; H, 6.57; N, 18.26; O, 12.52


Synonym: EPZ015666; EPZ-015666; EPZ 015666; GSK3235025; GSK-3235025; GSK 3235025.

IUPAC/Chemical Name: (S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N

InChi Code: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1

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


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

Safety Data Sheet (SDS):

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 C for short term (days to weeks) or -20 C 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 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Rioux N, Duncan KW, Lantz RJ, Miao X, Chan-Penebre E, Moyer MP, Munchhof MJ,
Copeland RA, Chesworth R, Waters NJ. Species differences in metabolism of
EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5)
inhibitor. Xenobiotica. 2015 Aug 21:1-10. [Epub ahead of print] PubMed PMID:
26294260.

2: Rioux N, Duncan KW, Lantz RJ, Miao X, Chan-Penebre E, Moyer MP, Munchhof MJ,
Copeland RA, Chesworth R, Waters NJ. Species differences in metabolism of
EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5)
inhibitor. Xenobiotica. 2015 Jul 31:1-10. [Epub ahead of print] PubMed PMID:
26228443.

3: Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston
LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K,
Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O,
Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland
RA, Chesworth R, Duncan KW. A selective inhibitor of PRMT5 with in vivo and in
vitro potency in MCL models. Nat Chem Biol. 2015 Jun;11(6):432-7. doi:
10.1038/nchembio.1810. Epub 2015 Apr 27. PubMed PMID: 25915199.