| MDL | - |
|---|---|
| Molecular Weight | 393.38 |
| Molecular Formula | C18H14F3N3O2S |
| SMILES | NC1=NC=C(C2=CC=C(S(=O)(C)=O)C=C2)C=C1C3=CC=C(C(F)(F)F)N=C3 |
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (K d app =0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent [1] .
|
Plasmodium |
MMV390048 against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain) showed a steep inhibition curve with IC50 and IC90 values of 28 and 40 nM, respectively.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02230579 | Medicines for Malaria Venture|University of Cape Town |
Malaria
|
May 2014 | Phase 1 |
| NCT03195387 | Medicines for Malaria Venture|Datamap|PrimeVigilance Zagreb|ICON Clinical Research|Sanaria Inc.|PTx Solutions Ltd., UK|University of Cape Town |
Malaria,Falciparum
|
January 2018 | Phase 1 |
| NCT02783833 | Medicines for Malaria Venture|Clinical Network Services (CNS) Pty Ltd|Q-Pharm Pty Limited|QIMR Berghofer Medical Research Institute |
Malaria
|
May 2016 | Phase 1|Phase 2 |
| NCT02281344 | Medicines for Malaria Venture|Q-Pharm Pty Limited |
Malaria, Falciparum
|
October 2014 | Phase 1 |
| NCT02880241 | Medicines for Malaria Venture|University of Gondar|Jimma University |
Malaria
|
October 20, 2017 | Phase 2 |
| NCT02554799 | Medicines for Malaria Venture|Richmond Pharmacology Limited |
Malaria
|
September 17, 2015 | Phase 1 |
| NCT02783820 | Medicines for Malaria Venture|Clinical Network Services (CNS) Pty Ltd|Q-Pharm Pty Limited|QIMR Berghofer Medical Research Institute |
Malaria
|
May 2016 | Phase 1 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
DMSO : 100 mg/mL ( 254.21 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5421 mL | 12.7104 mL | 25.4207 mL |
| 5 mM | 0.5084 mL | 2.5421 mL | 5.0841 mL |
| 10 mM | 0.2542 mL | 1.2710 mL | 2.5421 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution