MedKoo Cat#: 408024 | Name: GSK3368715 free base
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Description:

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

GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines.

Chemical Structure

GSK3368715 free base
GSK3368715 free base
CAS#1629013-22-4 (free base)

Theoretical Analysis

MedKoo Cat#: 408024

Name: GSK3368715 free base

CAS#: 1629013-22-4 (free base)

Chemical Formula: C20H38N4O2

Exact Mass: 366.2995

Molecular Weight: 366.55

Elemental Analysis: C, 65.54; H, 10.45; N, 15.29; O, 8.73

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 600.00 2 Weeks
25mg USD 1,150.00 2 Weeks
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Related CAS #
1628925-77-8 (2HCl) 2227587-25-7 (HCl) 2227587-26-8 (3HCl) 1629013-22-4 (free base)
Synonym
GSK3368715; GSK-3368715; GSK 3368715; EPZ019997; EPZ-019997; EPZ 019997; GSK3368715 free base; NSC823806; NSC 823806; NSC-823806
IUPAC/Chemical Name
N1-((3-(4,4-bis(ethoxymethyl)cyclohexyl)-1H-pyrazol-4-yl)methyl)-N1,N2-dimethylethane-1,2-diamine
InChi Key
SPEGERVLTUWZPA-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H38N4O2/c1-5-25-15-20(16-26-6-2)9-7-17(8-10-20)19-18(13-22-23-19)14-24(4)12-11-21-3/h13,17,21H,5-12,14-16H2,1-4H3,(H,22,23)
SMILES Code
CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C
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 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 366.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Noto PB, Sikorski TW, Zappacosta F, Wagner CD, Montes de Oca R, Szapacs ME, Annan RS, Liu Y, McHugh CF, Mohammad HP, Piccoli SP, Creasy CL. Identification of hnRNP-A1 as a pharmacodynamic biomarker of type I PRMT inhibition in blood and tumor tissues. Sci Rep. 2020 Dec 17;10(1):22155. doi: 10.1038/s41598-020-78800-6. PMID: 33335114; PMCID: PMC7746746. 2: Srour N, Mersaoui SY, Richard S. M-TAP Dance: Targeting PRMT1 and PRMT5 Family Members to Push Cancer Cells Over the Edge. Cancer Cell. 2019 Jul 8;36(1):3-5. doi: 10.1016/j.ccell.2019.06.004. PMID: 31287990. 3: Fedoriw A, Rajapurkar SR, O'Brien S, Gerhart SV, Mitchell LH, Adams ND, Rioux N, Lingaraj T, Ribich SA, Pappalardi MB, Shah N, Laraio J, Liu Y, Butticello M, Carpenter CL, Creasy C, Korenchuk S, McCabe MT, McHugh CF, Nagarajan R, Wagner C, Zappacosta F, Annan R, Concha NO, Thomas RA, Hart TK, Smith JJ, Copeland RA, Moyer MP, Campbell J, Stickland K, Mills J, Jacques-O'Hagan S, Allain C, Johnston D, Raimondi A, Porter Scott M, Waters N, Swinger K, Boriack-Sjodin A, Riera T, Shapiro G, Chesworth R, Prinjha RK, Kruger RG, Barbash O, Mohammad HP. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25. doi: 10.1016/j.ccell.2019.05.014. Epub 2019 Jun 27. PMID: 31257072. 4: Li X, Wang C, Jiang H, Luo C. A patent review of arginine methyltransferase inhibitors (2010-2018). Expert Opin Ther Pat. 2019 Feb;29(2):97-114. doi: 10.1080/13543776.2019.1567711. PMID: 30640571.