| Identification | Back Directory | [Name]
M-5717 | [CAS]
1469439-69-7 | [Synonyms]
M-5717
DDD107498
DDD107498 succinate
4-Quinolinecarboxamide, 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]- | [Molecular Formula]
C27H31FN4O2 | [MOL File]
1469439-69-7.mol | [Molecular Weight]
462.56 |
| Chemical Properties | Back Directory | [Boiling point ]
649.5±55.0 °C(Predicted) | [density ]
1.229±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥14.05 mg/mL in DMSO; ≥96 mg/mL in EtOH | [form ]
solid | [pka]
12.76±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1]. | [in vivo]
Cabamiquine (p.o., a single dose) shows an ED90 (90% reduction in parasitaemia) of 0.57 mg/kg in mice infected with the rodent parasiteP. berghei[1].
Cabamiquine (p.o., 3 mg/kg) shows Cmax of 80 ng/mL, Tmax of 4 h, AUC of 200542 ng·min/mL, F (%) of 84%[2].
| [IC 50]
CaMK III; Plasmodium | [storage]
Store at -20°C | [References]
[1] Baraga?a B, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20. DOI:10.1038/nature14451
[2] Baraga?a B, et al. Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy. J Med Chem. 2016 Nov 10;59(21):9672-9685. |
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