2377604-81-2
2377604-81-2 structure
- Name: CHMFL-PI4K-127
- Chemical Name: CHMFL-PI4K-127
- CAS Number: 2377604-81-2
- Molecular Formula: C18H15ClN4O3S
- Molecular Weight: 402.85
- Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
- Create Date: 2022-08-31 20:16:58
- Modify Date: 2023-02-03 07:34:05
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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[1].
| Name | CHMFL-PI4K-127 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
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) |
| In Vitro | 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]. |
| In Vivo | CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model[1]. 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. |
| References |
| Molecular Formula | C18H15ClN4O3S |
|---|---|
| Molecular Weight | 402.85 |