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| Product Name: | M-5717 | | Synonyms: | M-5717;DDD107498 succinate;DDD107498;4-Quinolinecarboxamide, 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-;6-fluoro-2-(4-(morpholinomethyl)phenyl)-N-(2-(pyrrolidin-1-yl)ethyl)quinoline-4-carboxamide;Cabamiquine(DDD107498;DDD107498,DDD 107498,DDD-498,protein,Calmodulin-dependent kinases,synthesis,antimalarial,stage,eEF2,DDD-107498,infection,Inhibitor,CaMK,multiple,Calmodulin-dependent protein kinases,DDD 498,M-5717,inhibit,M5717,Parasite;CID 71748268 | | CAS: | 1469439-69-7 | | MF: | C27H31FN4O2 | | MW: | 462.56 | | EINECS: | | | Product Categories: | | | Mol File: | 1469439-69-7.mol |  |
| | M-5717 Chemical Properties |
| 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 |
| | M-5717 Usage And Synthesis |
| 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 | | References | [1] Baragaa 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] Baragaa 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. |
| | M-5717 Preparation Products And Raw materials |
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