2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. NSC23925

NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.

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

NSC23925 Chemical Structure

NSC23925 Chemical Structure

CAS No. : 858474-14-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
1 mg USD 32 In-stock
5 mg USD 80 In-stock
10 mg USD 140 In-stock
25 mg USD 320 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

NSC23925 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.

IC50 & Target

P-glycoprotein[1]
In Vitro

NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor. SKOV-3 cells with long-term exposure of 1 μM NSC23925 show stable growth in culture medium. NSC23925 specifically inhibits Pgp overexpression to prevent the emergence of paclitaxel resistance during paclitaxel treatment[1]. NSC23925 reverses chemoresistance in a wide variety of tumor types where Multidrug resistance 1 (MDR1) is highly expressed. Maximal reversal of MDR is typically seen in NSC23925 doses between 0.5 and 1 μM. The IC50 for NSC23925 is 8 μM in SKOV-3/SKOV-3TR and 25 μM in OVCAR8/OVCAR8TR cell lines, whereas the mean concentration of NSC23925 required for maximal reversal of resistance in SKOV-3TR or OVCAR8TR to cytotoxic drugs is 0.5 μM to 1 μM[2].

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

NSC23925 Related Antibodies
In Vivo

Both saline alone and NSC23925 alone treated tumors grow progressively. The usage of NSC23925 in paclitaxel chemotherapy significantly prolongs anticancer efficacy of paclitaxel[1].

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

421.36

Formula

C22H26Cl2N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC(C1NCCCC1)C2=CC(C3=CC=C(OC)C=C3)=NC4=CC=CC=C24.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (33.91 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 4 mg/mL (9.49 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3733 mL 11.8663 mL 23.7327 mL
5 mM 0.4747 mL 2.3733 mL 4.7465 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 1.43 mg/mL (3.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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 (sealed storage, away from moisture)

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: 99.43%

COA (255 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

To determine whether NSC23925 can prevent the emergence of paclitaxel resistance, paclitaxel resistant ovarian cancer cells are used. In brief, 1×105 SKOV-3 cells are suspended in culture media containing paclitaxel alone, 1 μM NSC23925 alone, or paclitaxel in combination with 1 μM NSC23925. When the cells are cultured to 90% confluence, 1×105 cells are reseeded in a new tissue culture flask, and the paclitaxel dose is increased stepwise. The initial concentration of paclitaxel is 0.0001 μM. At different selection points cell sublines are collected and stored at liquid nitrogen for further analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Nude female mice at approximately 3 to 4 weeks of age are used. To evaluate the effects of NSC23925 on the induction of paclitaxel resistance in vivo, the paclitaxel resistant cells are established in human ovarian cancer xenograft models. Briefly, on day 1, approximately 2×106 parental sensitive SKOV-3 cells are injected subcutaneously with Matrigel into the flanks of 3 to 4-week-old female nude mice. Administration is initiated 12 days after injection of tumor cells. The mice are randomized into 4 groups and treated intraperitoneally with either saline alone, NSC23925 alone (50 mg/kg), paclitaxel (25 mg/kg) alone, or paclitaxel (25 mg/kg) in combination with NSC23925 (50 mg/kg) twice per week for 3 weeks followed by a treatment-free interval of 2 weeks. The second round of treatment is then continued. The size of tumors is recorded twice a week beginning on day 13. Tumor volume is measured with a digital caliper and calculated according to the formula (length×width2)/2[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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). 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
H2O / DMSO 1 mM 2.3733 mL 11.8663 mL 23.7327 mL 59.3317 mL
5 mM 0.4747 mL 2.3733 mL 4.7465 mL 11.8663 mL
DMSO 10 mM 0.2373 mL 1.1866 mL 2.3733 mL 5.9332 mL
15 mM 0.1582 mL 0.7911 mL 1.5822 mL 3.9554 mL
20 mM 0.1187 mL 0.5933 mL 1.1866 mL 2.9666 mL
25 mM 0.0949 mL 0.4747 mL 0.9493 mL 2.3733 mL
30 mM 0.0791 mL 0.3955 mL 0.7911 mL 1.9777 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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NSC23925 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:

NSC23925858474-14-3NSC 23925NSC-23925P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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