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GSK3368715 dihydrochloride
CAS No. 1628925-77-8
GSK3368715 dihydrochloride( —— )
Catalog No. M32952 CAS No. 1628925-77-8
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 89 | In Stock |
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| 2MG | 85 | In Stock |
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| 100MG | Get Quote | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGSK3368715 dihydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionGSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.
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DescriptionGSK3368715 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.
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In VitroGSK3368715 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.
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In VivoGSK3368715 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.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorHistone Methyltransferase
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Research Area——
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Indication——
Chemical Information
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CAS Number1628925-77-8
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Formula Weight439.46
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Molecular FormulaC20H40Cl2N4O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 230 mg/mL (523.37 mM; Ultrasonic ) H2O : 140 mg/mL (318.57 mM; Ultrasonic)
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SMILESCl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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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