[CAS NO. 1450666-80-4] UCT943
PRODUCTS SPECIFICATIONS [1450666-80-4]
DESCRIPTION [1450666-80-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 427.42 |
| Molecular Formula | C22H20F3N5O |
| SMILES | FC(F)(F)C1=CC=C(C2=NC(C3=CC=C(C(N4CCNCC4)=O)C=C3)=CN=C2N)C=C1 |
Summary
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K ( Pv PI4K) enzyme with an IC 50 of 23 nM [1] .
IC50 & Target
|
Pv PI4K 23 nM (IC 50 ) |
Plasmodium
|
In Vitro
UCT943 maintains high in vitro selectivity (>200-fold) for the parasite
Pv
PI4K versus the human PI4Kβ isozyme (IC
50
of PI4Kβ, 5.4 μM), inhibition of which is linked to immunosuppressive effects
[1]
.
In vitro cytotoxicity of UCT943 is tested against L6 cells, chinese hamster ovarian (CHO), Vero, and HepG2 cells, with 50% cytotoxic concentrations (CC
50
s) of 12, 17, 113, and 13 μM, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
UCT943 shows excellent in vivo efficacy in the Plasmodium berghei (10 mg/kg and 3 mg/kg; oral administration; daily; 4 days) and P. falciparum NSG (NOD- scid IL-2Rγ null ) mouse models (0.01, 0.1, 0.3, 1.1 and 10 mg/kg; oral administration; once per day; 4 days). When dosed at 10 mg/kg per os (p.o.), UCT943 reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice, with >30 mean survival days (MSD). At 3 mg/kg p.o., no complete cure is achieved, and MSD is 10 days, albeit parasitemia is reduced by 99%. The resulting 90% effective dose (ED 90 ) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED 90 is 0.25 mg/kg in the P. falciparum -infected NSG mouse model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mice with P. berghei and P. falciparum NOD- scid IL-2Rγ null (NSG) models [1] |
| Dosage: | 10 mg/kg and 3 mg/kg for P. berghei model; 0.01, 0.1, 0.3, 1.1 and 10 mg/kg for P. falciparum NOD- scid IL-2Rγ null (NSG) model |
| Administration: |
Oral administration; daily; 4 days for
P. berghei
model
Oral administration; once per day; 4 days for P. falciparum NOD- scid IL-2Rγ null (NSG) model |
| Result: | The ED 90 is 1.0 mg/kg in the P. berghei infection model. The ED 90 is 0.25 mg/kg in the P. falciparum -infected NSG mouse model. |
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 : 250 mg/mL ( 584.90 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3396 mL | 11.6981 mL | 23.3962 mL |
| 5 mM | 0.4679 mL | 2.3396 mL | 4.6792 mL |
| 10 mM | 0.2340 mL | 1.1698 mL | 2.3396 mL |