2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. Intoplicine dimesylate

Intoplicine dimesylate  (Synonyms: RP 60475 dimesylate)

Cat. No.: HY-101647A Purity: 98.28%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

Help & FAQs

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.

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

Intoplicine dimesylate Chemical Structure

Intoplicine dimesylate Chemical Structure

CAS No. : 133711-99-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 700 In-stock
Solution
10 mM * 1 mL in DMSO USD 737 In-stock
Solid
5 mg USD 620 In-stock
10 mg USD 1020 In-stock
25 mg USD 2050 In-stock
50 mg USD 3300 In-stock
100 mg USD 5300 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

Other Forms of Intoplicine dimesylate:

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Topoisomerase Topo I Topo II

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

In Vitro

With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2].
With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2].
Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure[2].

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

At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3[3].

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

540.65

Formula

C23H32N4O7S2
CAS No.
Appearance

Solid

Color

Light blue to blue

SMILES

OC1=CC=C2C3=C(NC4=C3C(NCCCN(C)C)=NC=C4C)C=CC2=C1.CS(O)(=O)=O.CS(O)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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 : 115 mg/mL (212.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (184.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8496 mL 9.2481 mL 18.4963 mL
5 mM 0.3699 mL 1.8496 mL 3.6993 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.

* 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: ≥ 5.75 mg/mL (10.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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: ≥ 5.75 mg/mL (10.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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.
Purity & Documentation
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
H2O / DMSO 1 mM 1.8496 mL 9.2481 mL 18.4963 mL 46.2406 mL
5 mM 0.3699 mL 1.8496 mL 3.6993 mL 9.2481 mL
10 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6241 mL
15 mM 0.1233 mL 0.6165 mL 1.2331 mL 3.0827 mL
20 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3120 mL
25 mM 0.0740 mL 0.3699 mL 0.7399 mL 1.8496 mL
30 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5414 mL
40 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
50 mM 0.0370 mL 0.1850 mL 0.3699 mL 0.9248 mL
60 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
80 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
100 mM 0.0185 mL 0.0925 mL 0.1850 mL 0.4624 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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Intoplicine dimesylate Related Classifications

Help & FAQs
  • How should lyophilized recombinant proteins be reconstituted and stored?

    1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss. 2. Taking 10 μg as an example, first add 20 μL of reconstituted solution provided by MCE and use a pipette to gently resuspend the lyophilized protein until it is fully dissolved.. (For most proteins, the reconstitution solution we provide is sterile water. If a diluent other than water is required, it will be indicated in the product's Certificate of Analysis (COA).). 3. Add an additional 80 μL of buffer/culture medium containing carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% trehalose), and then use a pipette to gently mix until uniform. The final concentration is should not be lower than 100 μg/mL. 4. Aliquot at least 20 μL per tube. 5. After aliquoting, store it frozen at a temperature ranging from -20ºC to -80ºC, and it can be preserved for 3 to 6 months.

  • How should solution-form recombinant proteins be stored?

    1. The product can be stored in its original form and diluted as needed upon use. 2. Alternatively, dilute with a buffer/culture medium containing a carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% alginate), mix well by pipetting, and ensure that

  • Why is it necessary to add carrier proteins?

    Carrier proteins are commonly added to enhance the stability of recombinant proteins, preventing them from adhering to the walls of the container during freezing or thawing processes. Plastic tubes have a certain adsorptive capacity for proteins, which may lead to difficulty in separating the protein from the tube walls, resulting in a decrease in the actual concentration of the protein in the solution and thus affecting its activity. To minimize such losses, it is recommended to add a commonly used carrier protein solution prior to the long-term storage of recombinant protein products.

  • Carrier protein types and options?

    In cases where the carrier protein is not expected to influence the experimental outcomes, an appropriate carrier protein, such as 0.1% BSA (Bovine Serum Albumin), 5% HSA (Human Serum Albumin), 10% FBS (Fetal Bovine Serum), or 5% trehalose, can be incorpo

Keywords:

Intoplicine dimesylate133711-99-6RP 60475 dimesylateTopoisomeraseantitumorbenzopyridoindoleInhibitorinhibitorinhibit

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