Tafenoquine|SB-252263;Tafenoquine;WR 238605

Cas No.:	106635-80-7
Chemical Name:	Tafenoquine free base
Synonyms:	1,4-Pentanediamine,N4-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]-8-quinolinyl]-;4-N-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine;Tafenoquine succinate;(RS)-N(sup 3)-(2,6-Dimethoxy-4-methyl-5-(3-trifluoro-methylphenoxy)quinolin-8-yl)pentane-1,4-diamine;1,4-Pentanediamine, N4-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)-8-quinolinyl)-;8-< (4-amino-1-methylbutyl)amino> -2,6-dimethoxy-4-methyl-5-< 3-(trifluoromethyl)phenoxy> quinoline;N(4)-(2,6-Dimethoxy-4-methyl-5-((3-trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine;Tafenoquine (USAN);Tafenoquine;4-[5-[3-(Trifluoromethyl)phenoxy]-2,6-dimethoxy-4-methyl-8-quinolinylamino]-1-pentanamine;N4-{2,6-Dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]-8-quinolinyl}-1,4-pentanediamine;N4-(2,6-diMethoxy-4-Methyl-5-(3-(trifluoroMethyl)phenoxy)quinolin-8-yl)pentane-1,4-diaMine;8-[(4-Amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinoline
SMILES:	CC1=CC(OC)=NC2=C1C(OC3=CC=CC(C(F)(F)F)=C3)=C(OC)C=C2NC(CCCN)C
Formula:	C₂₄H₂₈F₃N₃O₃
M.Wt:	463.501
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Tafenoquine (SB-252263, Tafenoquine, WR 238605) is a long-acting, orally active anti-malarial agent to prevent malaria that is holoendemic for Plasmodium falciparum.Parasite InfectionPhase 3 Clinical
Target:	Anti-malarial[1]
In Vivo:	Tafenoquine exhibits no anti-malarial activity in CYP 2D knock-out mice when dosed at their ED100 values (3 mg/kg) established in WT mice. Tafenoquine anti-malarial activity is partially restored in humanized/CYP 2D6 knock-in mice when tested at two times its ED100 (6 mg/kg)[1].
References:	[1]. Marcsisin SR, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J. 2014 Jan 3;13:2.

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