GSK3368715 dihydrochloride


Catalog No. Size PriceQuantity
M18518-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

Product information

CAS Number: 1628925-77-8

Molecular Weight: 439.46

Formula: C20H40Cl2N4O2

Chemical Name: ({3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)(methyl)[2-(methylamino)ethyl]amine dihydrochloride

Smiles: Cl.Cl.CNCCN(C)CC1=CNN=C1C1CCC(COCC)(COCC)CC1

InChiKey: HPSRPMOJFMXEKS-UHFFFAOYSA-N

InChi: InChI=1S/C20H38N4O2.2ClH/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);2*1H

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 230 mg/mL (523.37 mM; Need ultrasonic). H2O : 140 mg/mL (318.57 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.

In Vivo:

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively.

Products are for research use only. Not for human use.

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