ChemicalBook--->CAS DataBase List--->106635-81-8

106635-81-8

106635-81-8 Structure

106635-81-8 Structure
IdentificationBack Directory
[Name]

TAFENOQUINE SUCCINATE
[CAS]

106635-81-8
[Synonyms]

WR-238605
SB-252263
Krintafel
SB 252263AX
Wr238605 succinate
Tafenoquine Succinate
N-[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 succinate
TAFENOQUINE SUCCINATE; WR-238605, WR 238605, WR238605, SB-252263-AAB; SB252263-AAB; SB 252263-AAB; KRINTAFEL;
Butanedioic acid, compd. with N(sup 4)-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine (1:1)
[Molecular Formula]

C28H34F3N3O7
[MDL Number]

MFCD00892249
[MOL File]

106635-81-8.mol
[Molecular Weight]

581.581
Chemical PropertiesBack Directory
[Melting point ]

146-149°
[storage temp. ]

2-8°C
[solubility ]

DMSO: soluble5mg/mL (clear solution)
[form ]

powder
[color ]

white to beige
[InChIKey]

CQBKFGJRAOXYIP-UHFFFAOYSA-N
[SMILES]

OC(=O)CCC(O)=O.COc1cc(C)c2c(Oc3cccc(c3)C(F)(F)F)c(OC)cc(NC(C)CCCN)c2n1
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
[WGK Germany ]

3
[Storage Class]

11 - Combustible Solids
[Toxicity]

LD50 in male, female rats (mg/kg): 102, 71 i.p.; 429, 416 orally (LaMontagne)
Hazard InformationBack Directory
[Uses]

Tafenoquine succinate is a new 8-aminoquinoline with an improved therapeutic index and safety profile as compared to primaquine (P733500).Tafenoquine has the potential to become a widely used drug in the preven tion and treatment of malaria infection and could replace some currently used drugs as resistant strains of Plasmodium species increase.
[Biochem/physiol Actions]

Tafenoquine is an antimalarial primaquine analog being investigated to treat and prevent Plasmodium vivax infections. It can eliminate both blood and liver stages of Plasmodium vivax. Tafenoquine has also been tested as a therapy for leishmaniasis.
[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].

[IC 50]

Plasmodium
Spectrum DetailBack Directory
[Spectrum Detail]

TAFENOQUINE SUCCINATE(106635-81-8)1HNMR
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