1. Anti-infection Neuronal Signaling
  2. Parasite CaMK
  3. Cabamiquine

Cabamiquine  (Synonyms: DDD107498; DDD-498; M5717)

Cat. No.: HY-117684 Purity: 99.93%
SDS COA Handling Instructions

Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.

For research use only. We do not sell to patients.

Cabamiquine Chemical Structure

Cabamiquine Chemical Structure

CAS No. : 1469439-69-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 250 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1].

IC50 & Target

CaMK III

 

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
L6 IC50
28.47 μM
Compound: DDD107498
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue staining based fluorometric assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue staining based fluorometric assay
[PMID: 28279559]
MRC5 EC50
24 μM
Compound: 2; DDD107498
Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability after 68 hrs by resazurin dye based fluorescence assay
Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability after 68 hrs by resazurin dye based fluorescence assay
[PMID: 27631715]
In Vitro

Cabamiquine (24-48 h) leads to abnormal trophozoites, and inhibits the development of trophozoites and schizonts in parasites, and inhibits protein synthesis[1].
Cabamiquine shows excellent activity against 3D7 parasites: EC50 =1.0 nM, EC90 = 2.4 nM, EC99 = 5.9 nM[1].
Cabamiquine shows good metabolic stability when incubated with hepatic microsomes or hepatocyte[1].

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

In Vivo

Cabamiquine (p.o., a single dose) shows an ED90 (90% reduction in parasitaemia) of 0.57 mg/kg in mice infected with the rodent parasite P. berghei[1].
Cabamiquine (p.o., 3 mg/kg) shows Cmax of 80 ng/mL, Tmax of 4 h, AUC of 200542 ng·min/mL, F (%) of 84%[2].

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

Clinical Trial
Molecular Weight

462.56

Formula

C27H31FN4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C2=CC=C(C=C2)CN3CCOCC3)=NC4=CC=C(C=C41)F)NCCN5CCCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (216.19 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 2.1619 mL 10.8094 mL 21.6188 mL
5 mM 0.4324 mL 2.1619 mL 4.3238 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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 (protect from 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: 99.93%

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 (protect from 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 2.1619 mL 10.8094 mL 21.6188 mL 54.0470 mL
5 mM 0.4324 mL 2.1619 mL 4.3238 mL 10.8094 mL
10 mM 0.2162 mL 1.0809 mL 2.1619 mL 5.4047 mL
15 mM 0.1441 mL 0.7206 mL 1.4413 mL 3.6031 mL
20 mM 0.1081 mL 0.5405 mL 1.0809 mL 2.7024 mL
25 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1619 mL
30 mM 0.0721 mL 0.3603 mL 0.7206 mL 1.8016 mL
40 mM 0.0540 mL 0.2702 mL 0.5405 mL 1.3512 mL
50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0809 mL
60 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9008 mL
80 mM 0.0270 mL 0.1351 mL 0.2702 mL 0.6756 mL
100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5405 mL
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Cabamiquine 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.

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Cabamiquine
Cat. No.:
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