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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 2377604-81-2
- 分子式: C18H15ClN4O3S
- 分子量:402.85
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
|
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.
-
Animal Model:Balb/c mice were infected by P. yoelii[1].
-
Dosage:0, 60, 80 mg/kg
-
Administration:Orally, daily for 7 days
-
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.
-
Animal Model:Balb/c mice were infected by P. yoelii[1].
-
Dosage:0, 1, 5, 15 mg/kg
-
Administration:Orally, once
-
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.
化学情報
-
CAS 番号 2377604-81-2
-
性状 Solid
-
分子量 402.85
-
分子式 C18H15ClN4O3S
-
Color White to off-white
-
SMILES
O=C(C1=CN=CC(C2=CC(NS(=O)(C3=CC=CC=C3)=O)=C(Cl)N=C2)=C1)NC
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (274 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
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 |