CHMFL-PI4K-127
Based on 1 Customer Validation
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2377604-81-2
- Formula: C18H15ClN4O3S
- Molecular Weight:402.85
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
PI4K 0.9 ± 0.1 nM (IC50) |
PI3Kδ 104 ± 3 nM (IC50) |
PI3Kα 191 ± 36 nM (IC50) |
PI3Kγ 324 ± 19 nM (IC50) |
PI3Kβ 392 ± 27 nM (IC50) |
Vps34 681 ± 25 nM (IC50) |
CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase[1].
CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice were infected by P. yoelii[1].
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Dosage:0, 60, 80 mg/kg
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Administration:Orally, daily for 7 days
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Result:Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment.
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Animal Model:Balb/c mice were infected by P. yoelii[1].
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Dosage:0, 1, 5, 15 mg/kg
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Administration:Orally, once
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Result:Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy.
Chemical Information
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CAS No. 2377604-81-2
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Appearance Solid
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Molecular Weight 402.85
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Formula C18H15ClN4O3S
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Color White to off-white
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SMILES
O=C(C1=CN=CC(C2=CC(NS(=O)(C3=CC=CC=C3)=O)=C(Cl)N=C2)=C1)NC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (310.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4823 mL | 12.4116 mL | 24.8231 mL | 62.0578 mL |
| 5 mM | 0.4965 mL | 2.4823 mL | 4.9646 mL | 12.4116 mL | |
| 10 mM | 0.2482 mL | 1.2412 mL | 2.4823 mL | 6.2058 mL | |
| 15 mM | 0.1655 mL | 0.8274 mL | 1.6549 mL | 4.1372 mL | |
| 20 mM | 0.1241 mL | 0.6206 mL | 1.2412 mL | 3.1029 mL | |
| 25 mM | 0.0993 mL | 0.4965 mL | 0.9929 mL | 2.4823 mL | |
| 30 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0686 mL | |
| 40 mM | 0.0621 mL | 0.3103 mL | 0.6206 mL | 1.5514 mL | |
| 50 mM | 0.0496 mL | 0.2482 mL | 0.4965 mL | 1.2412 mL | |
| 60 mM | 0.0414 mL | 0.2069 mL | 0.4137 mL | 1.0343 mL | |
| 80 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL | |
| 100 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6206 mL |