Bioactivity | 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]. |
Invitro | 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]. Cell Viability Assay[3] Cell Line: |
Name | Halofantrine |
CAS | 69756-53-2 |
Formula | C26H30Cl2F3NO |
Molar Mass | 500.42 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [2]. H Tie, et al. Inhibition of HERG potassium channels by the antimalarial agent halofantrine. Br J Pharmacol. 2000 Aug;130(8):1967-75. [3]. Ji-Hyun Lee, et al. CDA: combinatorial drug discovery using transcriptional response modules. PLoS One. 2012;7(8):e42573. [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. |