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Benproperine phosphate

Cat No.:V75799 Purity: ≥98%
Benproperine phosphate is an orally bioactive and potent inhibitor of actin-associated protein 2/3 complex subunit 2 (ARPC2).
Benproperine phosphate
Benproperine phosphate Chemical Structure CAS No.: 19428-14-9
Product category: Arp2 3 Complex
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
Other Sizes
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Product Description
Benproperine phosphate is an orally bioactive and potent inhibitor of actin-associated protein 2/3 complex subunit 2 (ARPC2). Benproperine phosphate weakens the actin polymerization rate by impairing Arp2/3 function. Benproperine phosphate may be used to relieve cough and inhibit cancer cell migration and tumor metastasis.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In a dose-dependent manner, benproperine phosphate (20–120 μM) reduces cell viability for 24 hours [1]. Benproperine phosphate (10 μM; 24 hours of action) has an IC50 value of 1-2 μM and strongly inhibits the migration of different cancer cells, as well as the migration and invasion of DLD-1 and AsPC-1 cells. In MCF-10A cells, benproperine phosphate (10 μM; 24 hours) has no effect on cortactin-rich lamellipodia [1].
ln Vivo
The growth of primary pancreatic tumors is inhibited by benproperine phosphate (50, 100 mg/kg; oral gavage; 5 days per week for 4 weeks)[1]. Benproperine phosphate (56.1% inhibition) dramatically decreased the lung metastasis of mouse AsPC-1 cells. Benproperine phosphate reduced HCT-116 and DLD-1 cells' ability to spread to the liver by 78.9% and 78.2%, respectively[1].
Cell Assay
Cell Viability Assay[1]
Cell Types: DLD-1, AsPC-1, CFPAC-1, A375P, A375P, MDA-MB-231, DU145, DU145 cancer cells
Tested Concentrations: 20, 40, 60, 80, 100, 120 μM
Incubation Duration:For 24 hrs (hours)
Experimental Results: Inhibited cell viability in a dose-dependent manner.
Animal Protocol
Animal/Disease Models: Female BALB/c nude mice of 6weeks old with AsPC-1 cells[1]
Doses: 50, 100 mg/kg
Route of Administration: Oral gavage; 5 days per week for 4 weeks
Experimental Results: Inhibited primary pancreatic tumor growth compared to the vehicle control (47.7% inhibition) without body weights change.
References

[1]. Benproperine, an ARPC2 inhibitor, suppresses cancer cell migration and tumor metastasis. Biochem Pharmacol. 2019 May;163:46-59.

Additional Infomation
See also: Benproperine (annotation moved to).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H30NO5P
Molecular Weight
407.44
Exact Mass
407.186
CAS #
19428-14-9
PubChem CID
167811
Appearance
White to off-white solid powder
Boiling Point
433ºC at 760mmHg
Melting Point
148-153ºC
Vapour Pressure
1.06E-07mmHg at 25°C
LogP
3.539
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
6
Heavy Atom Count
28
Complexity
370
Defined Atom Stereocenter Count
0
InChi Key
MCVUURBOSHQXMK-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H27NO.H3O4P/c1-18(22-14-8-3-9-15-22)17-23-21-13-7-6-12-20(21)16-19-10-4-2-5-11-19;1-5(2,3)4/h2,4-7,10-13,18H,3,8-9,14-17H2,1H3;(H3,1,2,3,4)
Chemical Name
1-[1-(2-benzylphenoxy)propan-2-yl]piperidine;phosphoric acid
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, avoid exposure to moisture.
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: 125 mg/mL (306.79 mM)
H2O: ≥ 100 mg/mL (245.43 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.11 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 20.8 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: ≥ 2.08 mg/mL (5.11 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 20.8 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: ≥ 2.08 mg/mL (5.11 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 20.8 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 2.4543 mL 12.2717 mL 24.5435 mL
5 mM 0.4909 mL 2.4543 mL 4.9087 mL
10 mM 0.2454 mL 1.2272 mL 2.4543 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.

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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:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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