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GSK3368715 dihydrochloride

Catalog No. T11500L CAS 1628925-77-8

Synonyms: EPZ019997 dihydrochloride, GSK3368715 2HCl, EPZ019997 2HCl

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs) with anticancer and antitumor activity, inhibiting PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and can be used to study advanced solid tumors.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK3368715 dihydrochloride Chemical Structure

GSK3368715 dihydrochloride, CAS 1628925-77-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 79.00
5 mg	In stock	$ 128.00
100 mg	10-14 weeks	$ 812.00

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Purity: 99.66%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs) with anticancer and antitumor activity, inhibiting PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and can be used to study advanced solid tumors.
Targets&IC50	PRMT3:48 nM, PRMT1:3.1 nM, PRMT6:5.7 nM, PRMT4:1148 nM, PRMT8:1.7 nM
In vitro	In the majority of 249 cancer cell lines representing 12 tumor types, GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) exhibits 50% or more growth inhibition relative to DMSO-treated cells[1].
In vivo	GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) significantly affects the growth of BxPC3 xenografts at all doses tested. In the 150- and 300-mg/kg dose groups, it reduces tumor growth by 78% and 97%, respectively[1].

Synonyms	EPZ019997 dihydrochloride, GSK3368715 2HCl, EPZ019997 2HCl
Molecular Weight	439.46
Formula	C20H40Cl2N4O2
CAS No.	1628925-77-8

Storage

store at low temperature,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (227.55 mM), Sonication is recommended.

DMSO: 100 mg/mL (227.55 mM), Sonication is recommended.

References and Literature

1. Fedoriw A, et al. 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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK3368715 dihydrochloride 1628925-77-8 Chromatin/Epigenetic Histone Methyltransferase EPZ019997 dihydrochloride GSK 3368715 GSK-3368715 Dihydrochloride EPZ-019997 EPZ 019997 Dihydrochloride GSK-3368715 GSK3368715 2HCl GSK3368715 Dihydrochloride EPZ 019997 EPZ019997 EPZ019997 2HCl EPZ-019997 Dihydrochloride GSK 3368715 Dihydrochloride GSK3368715 inhibitor inhibit

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