2. PI3K/Akt/mTOR
  3. PI4K PI3K
  4. CHMFL-PI4K-127

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.

CHMFL-PI4K-127 Chemical Structure

CHMFL-PI4K-127 Chemical Structure

CAS No. : 2377604-81-2

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Customer Review

Based on 1 publication(s) in Google Scholar

CHMFL-PI4K-127 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CHMFL-PI4K-127 Related Antibodies
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].

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.
Molecular Weight

402.85

Formula

C18H15ClN4O3S
CAS No.
Appearance

Solid

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
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4823 mL 12.4116 mL 24.8231 mL
5 mM 0.4965 mL 2.4823 mL 4.9646 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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CHMFL-PI4K-127 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CHMFL-PI4K-1272377604-81-2PI4KPI3KPhosphatidylinositol 4 kinasesPI4 kinasesPhosphoinositide 3-kinasePI4K kinaseKinase inhibitorMalariaBlood stageLiver stageantimalariaInhibitorinhibitorinhibit

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