1. Epigenetics
  2. Histone Methyltransferase
  3. GSK3368715 dihydrochloride

GSK3368715 dihydrochloride (Synonyms: EPZ019997 dihydrochloride)

Cat. No.: HY-128717A Purity: 99.94%
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK3368715 dihydrochloride Chemical Structure

GSK3368715 dihydrochloride Chemical Structure

CAS No. : 1628925-77-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 145 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
Estimated Time of Arrival: December 31
100 mg USD 980 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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[1].

IC50 & Target

IC50: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)[1]
Kiapp: 1.5 nM (PRMT1), 81 nM (PRMT3), 19 nM (PRMT4), 2.4 nM (PRMT6), 2 nM (PRMT8)[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

439.46

Formula

C₂₀H₄₀Cl₂N₄O₂

CAS No.
SMILES

CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 230 mg/mL (523.37 mM; Need ultrasonic)

H2O : 140 mg/mL (318.57 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2755 mL 11.3776 mL 22.7552 mL
5 mM 0.4551 mL 2.2755 mL 4.5510 mL
10 mM 0.2276 mL 1.1378 mL 2.2755 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.94%

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Keywords:

GSK3368715EPZ019997GSK 3368715GSK-3368715EPZ 019997EPZ-019997Histone MethyltransferaseInhibitorinhibitorinhibit

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Product Name:
GSK3368715 dihydrochloride
Cat. No.:
HY-128717A
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