1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. 9-Aminocamptothecin

9-Aminocamptothecin  (Synonyms: 9-Amino-20(S)-camptothecin; 9-Amino-CPT)

Cat. No.: HY-100309 Purity: 99.05%
COA Handling Instructions

9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity.

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

9-Aminocamptothecin Chemical Structure

9-Aminocamptothecin Chemical Structure

CAS No. : 91421-43-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
2 mg USD 64 In-stock
5 mg USD 115 In-stock
10 mg USD 180 In-stock
25 mg USD 320 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 9-Aminocamptothecin

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity[1].

IC50 & Target[1]

Topoisomerase I

 

In Vitro

In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm[1]. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure[2].

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

In Vivo

9-Aminocamptothecin (9-Amino-CPT) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-Aminocamptothecin is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group[2]. 9-Aminocamptothecin induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML[3].

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

Molecular Weight

363.37

Formula

C20H17N3O4

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C(N)C=CC=C5N=C4C3=C2)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (9.16 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 2.7520 mL 13.7601 mL 27.5202 mL
5 mM 0.5504 mL 2.7520 mL 5.5040 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 0.33 mg/mL (0.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 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: ≥ 0.33 mg/mL (0.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 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).
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: 99.05%

References
Cell Assay
[1]

The cytotoxicity of 9-amino-CPT (9-amino-20(S)-camptothecin) is assessed by clonogenic assay. Exponentially growing cells are resuspended in media, cell number is determined using an electronic counter, and 100–250 cells are inoculated in triplicate onto 60 15-mm dishes containing 5 mL of medium. After an overnight incubation, 5 μL of 9-Aminocamptothecin stock solutions are added to the dishes to achieve final concentrations of 0, 0.27, 1.37, 2.74, 13.7, 27.4, 137, and 274 nM. After 4-, 8-, 12-, 24-, 48-, 72-, and 240-h exposures, medium is removed by aspiration and fresh medium is added to the dishes. Percentage of survival at each drug concentration with different exposure time is determined from the ratio of the number of the colonies in the drug-treated sample:the number in the control (DMSO vehicle-treated) sample[1].

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

Animal Administration
[3]

Mice: Treatment with 9-Aminocamptothecin is started on day 7 after inoculation with KBM-3 cells. Five groups of 5 mice each (average weight of 22 g) are used and treatment is administered daily 4 days a week for 3 weeks as follows: 1) group 1 control mice are injected IV with PBS; 2) group 2 mice receive 1.33 mg/kg 9-Aminocamptothecin IV, 3) group 3 mice receive 1.33 mg/kg 9-Aminocamptothecin orally by gavage; 4) group 4 mice receive 2.0 mg/kg 9-Aminocamptothecin IV; 5) group 5 mice receive 2.0 mg/kg 9-Aminocamptothecin orally by gavage[3].

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. 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
DMSO 1 mM 2.7520 mL 13.7601 mL 27.5202 mL 68.8004 mL
5 mM 0.5504 mL 2.7520 mL 5.5040 mL 13.7601 mL
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9-Aminocamptothecin 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.

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9-Aminocamptothecin
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