Halofantrine  (Synonyms: 卤泛群; 卤方特瑞; SKF-102886 free base; WR-171669)

Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum^[1]. Halofantrine blocks HERG potassium channels^[2].

Halofantrine blocks HERG tail currents elicited on repolarization to 760 mV from +30 mV with an IC₅₀ of 196.9 nM^[2].
Halofantrine inhibits MDA-MB-231 triple-negative breast cancer (TNBC) cell proliferation with the IC₅₀ of 7.73±0.23 μM^[3].
Halofantrine exhibits activity against asexual forms (3D7A), asexual forms (3D7HT-GFP), and mature gametocytes IV-V with IC₅₀s of 0.0011, 0.0012, and 6.70 μM, respectively^[4].

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

500.42

C₂₆H₃₀Cl₂F₃NO

69756-53-2

氯氟菲醇；卤泛群；卤方特瑞

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. A J Humberstone, et al. Effect of altered serum lipid concentrations on the IC50 of halofantrine against Plasmodium falciparum. J Pharm Sci. 1998 Feb;87(2):256-8.  [Content Brief]

  [2]. H Tie, et al. Inhibition of HERG potassium channels by the antimalarial agent halofantrine. Br J Pharmacol. 2000 Aug;130(8):1967-75.  [Content Brief]

  [3]. Ji-Hyun Lee, et al. CDA: combinatorial drug discovery using transcriptional response modules. PLoS One. 2012;7(8):e42573.  [Content Brief]

  [4]. Joël Lelièvre, et al. Activity of clinically relevant antimalarial drugs on Plasmodium falciparum mature gametocytes in an ATP bioluminescence "transmission blocking" assay. PLoS One. 2012;7(4):e35019.  [Content Brief]