[CAS NO. 1513879-19-0] KDU691
PRODUCTS SPECIFICATIONS [1513879-19-0]
DESCRIPTION [1513879-19-0]
Overview
| MDL | MFCD28963927 |
|---|---|
| Molecular Weight | 419.86 |
| Molecular Formula | C22H18ClN5O2 |
| SMILES | ClC1=CC=C(N(C(C2=CN3C(C=N2)=NC=C3C4=CC=C(C(NC)=O)C=C4)=O)C)C=C1 |
Summary
KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites [1] .
IC50 & Target
|
Plasmodium |
In Vivo
During the 5 days of dosing, no major weight changes are observed in the animals that receive KDU691 as prophylactic treatment (group 691-proph). From the fourth day of dosing, the animals that are treated with KDU691 show a transient yellow skin color. The KDU691 radical-cure group (group 691-RC) becomes blood-stage positive again at 31.8 days p.i. (range, 31 to 32 days). Clinical chemistry analysis of the group 691-RC monkeys reveals that bilirubin levels accumulate during the 5-day radical-cure treatment with KDU691 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 150 mg/mL ( 357.26 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3817 mL | 11.9087 mL | 23.8175 mL |
| 5 mM | 0.4763 mL | 2.3817 mL | 4.7635 mL |
| 10 mM | 0.2382 mL | 1.1909 mL | 2.3817 mL |
References
- [1] Dembele L, et al. The Plasmodium PI(4)K inhibitor KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites. Sci Rep. 2017;7(1):2325. Published 2017 May 24.
- [2] Zeeman AM, et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites. Antimicrob Agents Chemother. 2016;60(5):2858-2863. Published 2016 Apr 22.