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Cabamiquine succinate (DDD107498 succinate; DDD-498 succinate; M5717 succinate)

Cat No.:V52993 Purity: ≥98%
Cabamiquine (DDD107498) succinate is a potent, orally bioavailable antimalarial agent that can inhibit multiple stages of the parasite life cycle, with EC50 of 1 nM against P. falciparum 3D7.
Cabamiquine succinate (DDD107498 succinate; DDD-498 succinate; M5717 succinate)
Cabamiquine succinate (DDD107498 succinate; DDD-498 succinate; M5717 succinate) Chemical Structure CAS No.: 2444781-71-7
Product category: CaMK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
Other Sizes

Other Forms of Cabamiquine succinate (DDD107498 succinate; DDD-498 succinate; M5717 succinate):

  • DDD107498
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Cabamiquine (DDD107498) succinate is a potent, orally bioavailable antimalarial agent that can inhibit multiple stages of the parasite life cycle, with EC50 of 1 nM against P. falciparum 3D7. Cabamiquine succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with EC50 of 2 nM for WT-PfeEF2.
Biological Activity I Assay Protocols (From Reference)
Targets
CaMK III Plasmodium
ln Vitro
Camiquine succinate (24–48 hours) disrupts protein synthesis, produces irregularities in trophozoites, and prevents the formation of trophozoites and fragmented aggregates in the parasite [1]. With EC50 = 1.0 nM, EC90 = 2.4 nM, and EC99 = 5.9 nM against 3D7 parasites, carbaquine succinate exhibits good efficacy[1]. When coupled with hepatocytes or liver microsomes, camelquin succinate shows good metabolic stability [1].
ln Vivo
Cabamiquine (DDD107498) exhibits an ED90 of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite P. berghei[1].
References

[1]. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20.

[2]. Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy. J Med Chem. 2016 Nov 10;59(21):9672-9685.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C31H37FN4O6
Molecular Weight
580.6471
Exact Mass
580.269
CAS #
2444781-71-7
Related CAS #
Cabamiquine;1469439-69-7
PubChem CID
138319698
Appearance
White to off-white solid powder
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
10
Heavy Atom Count
42
Complexity
739
Defined Atom Stereocenter Count
0
SMILES
FC1C([H])=C([H])C2=C(C=1[H])C(=C([H])C(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=N2)C(N([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O.O([H])C(C([H])([H])C([H])([H])C(=O)O[H])=O
InChi Key
OTKHBNSZSWWVRJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H31FN4O2.C4H6O4/c28-22-7-8-25-23(17-22)24(27(33)29-9-12-31-10-1-2-11-31)18-26(30-25)21-5-3-20(4-6-21)19-32-13-15-34-16-14-32;5-3(6)1-2-4(7)8/h3-8,17-18H,1-2,9-16,19H2,(H,29,33);1-2H2,(H,5,6)(H,7,8)
Chemical Name
butanedioic acid;6-fluoro-2-[4-(morpholin-4-ylmethyl)phenyl]-N-(2-pyrrolidin-1-ylethyl)quinoline-4-carboxamide
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 135 mg/mL (232.50 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.25 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.25 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.25 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7222 mL 8.6110 mL 17.2221 mL
5 mM 0.3444 mL 1.7222 mL 3.4444 mL
10 mM 0.1722 mL 0.8611 mL 1.7222 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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