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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Tafenoquine (formerly known as SB252263-AAB; WR-238605; WR238605; Brand name Krintafel) is an 8-aminoquinoline analog and oral drug developed by GlaxoSmithKline that has been investigated and approved in 2018 as a potential treatment for malaria, as well as for malaria prevention. In July 2018, United States Food and Drug Administration (US FDA) approved single dose tafenoquine for the radical cure (prevention of relapse) of Plasmodium vivax malaria. Tafenoquine targets leishmania respiratory complex III and induces apoptosis. Tafenoquine has a long half-life of approximately 14 days and is generally safe and well tolerated.
| Targets |
Anti-malarial
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|---|---|
| ln Vivo |
When tafenoquine is administered at the 3 mg/kg ED100 values that were established in WT mice, it shows no anti-malarial activity in CYP 2D knock-out mice. When tested at twice its ED100 (6 mg/kg), tafenoquine's anti-malarial activity is partially restored in humanized/CYP 2D6 knock-in mice[1].
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| References |
| Molecular Formula |
C24H28F3N3O3
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|---|---|
| Molecular Weight |
463.50
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| Exact Mass |
463.21
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| Elemental Analysis |
C, 62.19; H, 6.09; F, 12.30; N, 9.07; O, 10.36
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| CAS # |
106635-80-7
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| Related CAS # |
Tafenoquine Succinate;106635-81-8
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| Appearance |
Light yellow solid powder
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| SMILES |
CC1=CC(=NC2=C1C(=C(C=C2NC(C)CCCN)OC)OC3=CC=CC(=C3)C(F)(F)F)OC
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| InChi Key |
LBHLFPGPEGDCJG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28F3N3O3/c1-14-11-20(32-4)30-22-18(29-15(2)7-6-10-28)13-19(31-3)23(21(14)22)33-17-9-5-8-16(12-17)24(25,26)27/h5,8-9,11-13,15,29H,6-7,10,28H2,1-4H3
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| Chemical Name |
N4-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)quinolin-8-yl)pentane-1,4-diamine
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| Synonyms |
WR-238605, WR 238605, WR238605, SB-252263-AAB; SB252263-AAB; SB 252263-AAB; Tafenoquine; Krintafel
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~93 mg/mL ( ~200.65 mM )
Ethanol : ~93 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1575 mL | 10.7875 mL | 21.5750 mL | |
| 5 mM | 0.4315 mL | 2.1575 mL | 4.3150 mL | |
| 10 mM | 0.2157 mL | 1.0787 mL | 2.1575 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Schematic illustrating pitfalls and protections of suppressive (yellow dose indicators) or causal (orange dose indicators) chemoprevention of non-relapsing malaria likeP. falciparum(top panel; red triangles and squares for inoculation and attack, respectively) or relapsing species likeP. vivax(bottom panel; green triangles and squares).J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. |
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 Geographic distribution and prevalence ofP. vivax(A) andP. falciparum(B) in 2010,reproduced here under Creative Commons license.
Hypothesized relative attack rates in the months following radical cure illustrate possible impacts of variable risks of relapse or reinfection on the estimation hypnozoitocidal efficacy oftafenoquine(TQ) fixed at a presumed ‘actual’ 95% rate compared to a chloroquine (CQ) arm without hypnozoitocidal therapy (relapse and reinfection attacks).J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. |
 Antimalarial classes as guided by life cycle of the plasmodia.
Evolution of the 8-aminoquinoline hypnozoitocides, including the winnowing out of irreversible severe neurotoxicity of plasmocid and related compounds distinguished by fewer than four methylene groups separating the amino groups of the alkyl chain at the defining 8-amino position. Plasmochin and others (including primaquine) having at least four methylene groups exhibited no such neurotoxicity but instead reversible toxicity at sub-lethal doses involving principally hepatic, hematological and gastrointestinal systems.J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. |
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