2. Anti-infection Cell Cycle/DNA Damage Apoptosis
  3. Parasite DNA/RNA Synthesis Apoptosis
  4. Febrifugine dihydrochloride

Febrifugine dihydrochloride is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine dihydrochloride inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids.

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Febrifugine dihydrochloride Chemical Structure

Febrifugine dihydrochloride Chemical Structure

CAS No. : 32434-42-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Febrifugine dihydrochloride:

Febrifugine dihydrochloride Related Antibodies

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Description

Febrifugine dihydrochloride is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine dihydrochloride inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids[1][2][3].

IC50 & Target

Plasmodium

 

In Vitro

Febrifugine (7-70 nM; 90 minutes) dihydrochloride increases eIF2α phosphorylation in a dose-dependent manner in asynchronous P. falciparum Dd2 cultures[1].
Febrifugine dihydrochloride inhibits the asexual blood stage of the P. falciparum 3D7 parasite strain with an EC50 of 4.0 nM[1].
Febrifugine (0-0.225 μM; 48 h) dihydrochloride effectively inhibits the proliferation growth of bladder cancer cells T24 and SW780 with IC50 of 0.02 μM and 0.018 μM, respectively[3].
Febrifugine (0.05-0.2 μM; 24 h) dihydrochloride increases the number of cells in the G1 phase, and decreases the number in the G2 phase[3].
Febrifugine (0.05-0.15 μM) dihydrochloride inhibits cell proliferation by suppressing DNA synthesis and induces cell death by reducing steroidogenesis and promoting apoptosis[3].
Febrifugine (0.025 μM) dihydrochloride downregulates low density lipoprotein receptor-associated protein, lanosterol synthase, cholesterol biosynthesis second rate-limiting enzyme, 7-dehydrocholesterol reductase, flavin adenine dinucleotide dependent oxidoreductase and other factors to inhibit the production of intracellular steroids in bladder cancer T24 cells[3].

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

Febrifugine dihydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: Asynchronous P. falciparum Dd2 cultures
Concentration: 7 nM, 70 nM
Incubation Time: 90 minutes
Result: Increased the eIF2α phosphorylation.

Cell Viability Assay[3]

Cell Line: T24 and SW780 cells
Concentration: 0.05 μM , 0.1 μM , 0.15 μM , 0.2 μM , 0.225 μM
Incubation Time: 48 h
Result: Decreased the cell viability of bladder cancer cells.

Cell Cycle Analysis[3]

Cell Line: T24 cells
Concentration: 0.05 μM, 0.1 μM , 0.2 μM
Incubation Time: 24 h
Result: Revealed alterations in G1 and G2 progression.
In Vivo

Febrifugine (1 mg/kg/day; p.o.; once a day for 3 consecutive days before parasite infection) dihydrochloride significantly reduces the mortality and the level of parasitemia[2].
Febrifugine (0.1 mg/kg; once every 3 days; 10 doses) dihydrochloride effectively inhibits bladder cancer xenograft proliferation in BALB/c nude mice[3].

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

Animal Model: Male ICR mice (6 weeks of age) infected with erythrocytic stage Plasmodium berghei NK65[2].
Dosage: 1 mg/kg/day
Administration: p.o.; once a day for 3 consecutive days before parasite infection.
Result: Significantly reduced the mortality and the level of parasitemia.
Molecular Weight

374.26

Formula

C16H21Cl2N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC(C[C@H]2NCCC[C@@H]2O)=O)C=NC3=C1C=CC=C3.Cl.Cl
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (22.26 mM; ultrasonic and warming and heat to 60°C; 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 2.6719 mL 13.3597 mL 26.7194 mL
5 mM 0.5344 mL 2.6719 mL 5.3439 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 (sealed storage, away from moisture and light). 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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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.62 mg/mL (1.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.62 mg/mL (1.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

SDS (392 KB)

COA (250 KB) HNMR (253 KB) LCMS (92 KB)

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 (sealed storage, away from moisture and light). 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 2.6719 mL 13.3597 mL 26.7194 mL 66.7985 mL
5 mM 0.5344 mL 2.6719 mL 5.3439 mL 13.3597 mL
10 mM 0.2672 mL 1.3360 mL 2.6719 mL 6.6798 mL
15 mM 0.1781 mL 0.8906 mL 1.7813 mL 4.4532 mL
20 mM 0.1336 mL 0.6680 mL 1.3360 mL 3.3399 mL
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Febrifugine dihydrochloride 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:

Febrifugine32434-42-7ParasiteDNA/RNA SynthesisApoptosisQuinazolinonealkaloid antimalarialInhibitorinhibitorinhibit

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