2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. Namitecan

Namitecan is a potent topoisomerase I inhibitor, with antitumor property.

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

Namitecan Chemical Structure

Namitecan Chemical Structure

CAS No. : 372105-27-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 478 In-stock
Solution
10 mM * 1 mL in DMSO USD 478 In-stock
Solid
1 mg USD 245 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
50 mg USD 2550 In-stock
100 mg USD 4080 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Namitecan Related Antibodies

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Topoisomerase Topo I Topo II

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Namitecan is a potent topoisomerase I inhibitor, with antitumor property.

IC50 & Target[1]

Topoisomerase I

 

In Vitro

Namitecan and cetuximab cooperate in inhibiting EGFR expression. Namitecan induces a dose-dependent decrease in EGFR expression in the different cell lines[1]. ST1968 induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50 of 0.21 and 0.29 μM[2].

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

Namitecan Related Antibodies
In Vivo

Namitecan (10 mg/kg) in combination with cetuximab (1 mg/mouse) induces synergistic antitumor effects in SCC models as a function of EGFR gene copy number[1]. ST1968 (25 mg/kg) causes acceptable body weight loss and no toxic deaths. ST1968 produces a 100% complete response rate in the mice bearing the A431 tumor, and retains a relevant activity in the topotecan-resistant tumor[2].

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

434.44

Formula

C23H22N4O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(/C=N/OCCN)C5=CC=CC=C5N=C4C3=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (575.45 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 2.3018 mL 11.5091 mL 23.0181 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).
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
References
Cell Assay
[1]

The antiproliferative activity is evaluated after 72 hours of drug exposure by cell counting. Drug concentrations able to inhibit cell proliferation by 50% (IC50) and 20% (IC20) are calculated from dose-response curves.

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

To generate tumor xenografts, exponentially growing cells (A431 and A431/topotecan, 107 cells/mouse; SiHa 2.5 × 107 cells/mouse, Caski 107 cells/mouse) are s.c. injected into the mice flanks. For antitumor activity studies, groups of four/five mice bearing tumor implanted in both flanks are used. Tumor fragments are implanted on day 0, and tumor growth is followed by biweekly measurements of tumor diameters with a Vernier caliper. Tumor volume (TV) is calculated according to the formula TV (mm3) = d2 × D/2, in which d and D are the shortest and the longest diameter, respectively. Treatment starts 5 to 13 days after implant, when the tumors are just palpable, but established (TV = 80-90 mm3). Namitecan, irinotecan, and cetuximab are administered every fourth day for four times. Cetuximab is given 1 hour after each administration of the camptothecin.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3018 mL 11.5091 mL 23.0181 mL 57.5453 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 mL 11.5091 mL
10 mM 0.2302 mL 1.1509 mL 2.3018 mL 5.7545 mL
15 mM 0.1535 mL 0.7673 mL 1.5345 mL 3.8364 mL
20 mM 0.1151 mL 0.5755 mL 1.1509 mL 2.8773 mL
25 mM 0.0921 mL 0.4604 mL 0.9207 mL 2.3018 mL
30 mM 0.0767 mL 0.3836 mL 0.7673 mL 1.9182 mL
40 mM 0.0575 mL 0.2877 mL 0.5755 mL 1.4386 mL
50 mM 0.0460 mL 0.2302 mL 0.4604 mL 1.1509 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9591 mL
80 mM 0.0288 mL 0.1439 mL 0.2877 mL 0.7193 mL
100 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5755 mL
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Namitecan 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:

Namitecan372105-27-6ST-1968ST1968ST 1968TopoisomeraseInhibitorinhibitorinhibit

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