Halofantrine

Modify Date: 2024-01-21 11:11:53

Halofantrine Structure
Halofantrine structure
Common Name Halofantrine
CAS Number 69756-53-2 Molecular Weight 500.42400
Density 1.244 g/cm3 Boiling Point 596.2ºC at 760 mmHg
Molecular Formula C26H30Cl2F3NO Melting Point 136-138ºC
MSDS N/A Flash Point 314.4ºC

 Use of Halofantrine


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].

 Names

Name halofantrine
Synonym More Synonyms

 Halofantrine Biological Activity

Description 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].
Related Catalog
In Vitro 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: MDA-MB-231 TNBC Concentration: 0, 2.50, 5.00, 10.00, 20.00, 40.00, and 80.00 μM Incubation Time: 3 days Result: IC50 was 7.73±0.23 μM.
References

[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.

 Chemical & Physical Properties

Density 1.244 g/cm3
Boiling Point 596.2ºC at 760 mmHg
Melting Point 136-138ºC
Molecular Formula C26H30Cl2F3NO
Molecular Weight 500.42400
Flash Point 314.4ºC
Exact Mass 499.16600
PSA 23.47000
LogP 8.64430
Index of Refraction 1.577

 Synonyms

3-DIBUTYLAMINO-1-(1,3-DICHLORO-6-TRIFLUOROMETHYL-PHENANTHREN-9-YL)-PROPAN-1-OL HCL
Halofan
1,3-dichloro-6-trifluoromethyl-9-[1-hydroxy-3-(dibutylamino)-propyl]-phenanthrene
3-(Dibutylamino)-1-(1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl)propan-1-ol