| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PI4Kβ-IN-1 (Compound 18) potently inhibited recombinant Plasmodium vivax phosphatidylinositol 4-kinase IIIβ (PvPI4K) in the presence of ATP, with an IC50 value of 1.2 nM[1]. PI4Kβ-IN-1 (96 h) showed potent antimalarial activity against Plasmodium falciparum asexual blood stage (ABS) parasites, with IC50 values of 0.024 μM (NF54, drug-sensitive strain) and 0.053 μM (K1, multidrug-resistant strain), respectively[1]. PI4Kβ-IN-1 also showed killing activity against Plasmodium falciparum gametophytes, with IC50 values of 0.38 μM (immature gametophytes) and 0.61 μM (late gametophytes), respectively[1]. PI4Kβ-IN-1 inhibits Plasmodium falciparum liver schizonts (IC50 = 0.065 μM) and blocks Plasmodium falciparum gamete formation (IC50 = 0.87 μM)[1]. PI4Kβ-IN-1 exhibits low cytotoxicity to mammalian cells, with IC50 values of 30 μM (CHO cells), 18.2 μM (HepG2 cells), and 47.8 μM (L6 cells), respectively[1]. PI4Kβ-IN-1 inhibits human ataxia-telangiectasia mutant kinase (HsATM), with IC50 values of 2 nM (10 μM ATP) and 103 nM (500 μM ATP), respectively[1].
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|---|---|
| ln Vivo |
PI4Kβ-IN-1 (Compound 18) (1-30 mg/kg, interface, once daily for 4 days) showed potent anti-topological activity in a humanized NOD-scid IL-2Rγnull (NSG) mouse model infected with Plasmodium falciparum Pf3D70087/N9 [1].
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| Animal Protocol |
Animal/Disease Models: Plasmodium falciparum Pf3D70087/N9 parasites were intravenously or intraperitoneally administered to 6-week-old (or relevant age) immunodeficient NOD-scid IL-2Rγnull (NSG) mice to construct the humanized mouse malaria infection model[1]
Doses: 1, 3, 10, 30 mg/kg Route of Administration: p.o., once daily, 4 consecutive days Experimental Results: Achieved an effective dose for 90% reduction in parasitemia (ED90) of 4.6 mg/kg. |
| References |
| Molecular Formula |
C22H22N4O2
|
|---|---|
| Molecular Weight |
374.44
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6707 mL | 13.3533 mL | 26.7065 mL | |
| 5 mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | |
| 10 mM | 0.2671 mL | 1.3353 mL | 2.6707 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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