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

Name: 9-Aminocamptothecin
Brand: MedChemExpress
SKU: HY-100309
Rating: 4.5 (1 reviews)

Cat. No.: HY-100309 Purity: 98.80%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 91421-43-1

Size	Price	Stock	Quantity
2 mg	USD 64	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE 9-Aminocamptothecin

•Research Square Preprint. 2024 Feb 23.

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Topoisomerase Topo I Topo II

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

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	1 nM Compound: 9	Cytotoxicity against mouse bone marrow cell by CFU-GM assay Cytotoxicity against mouse bone marrow cell by CFU-GM assay	[PMID: 21341674]
Bone marrow cell	IC₅₀	90 nM Compound: 9	Cytotoxicity against human bone marrow cell by CFU-GM assay Cytotoxicity against human bone marrow cell by CFU-GM assay	[PMID: 21341674]
HL-60	IC₅₀	0.11 μM Compound: 5g	Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells	[PMID: 8410981]
L1210	IC₅₀	12.7 nM Compound: 2	Concentration required to inhibit 50% of cell growth in L1210 murine leukemia cell line after 48 hr continuous treatment Concentration required to inhibit 50% of cell growth in L1210 murine leukemia cell line after 48 hr continuous treatment	10.1016/S0960-894X(97)00105-4

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.

91421-43-1

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
10 mM	---	---	---

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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.33 mg/mL (0.91 mM); Clear solution

This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 98.89%

Select Batch:

Data Sheet (280 KB) SDS (479 KB)

COA (255 KB) RP-HPLC (141 KB) LCMS (482 KB)

Handling Instructions (2659 KB)

References

[1]. Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74. [Content Brief]

[2]. de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94. [Content Brief]

[3]. Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64. [Content Brief]

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	[1]. Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74. [Content Brief] [2]. de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94. [Content Brief] [3]. Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64. [Content Brief]

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.5504 mL	2.7520 mL	5.5040 mL	13.7601 mL

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.

Keywords:

9-Aminocamptothecin91421-43-19-Amino-20(S)-camptothecin 9-Amino-CPTTopoisomeraseInhibitorinhibitorinhibit

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

Customer Review

9-Aminocamptothecin Related Antibodies

1 Publications Citing Use of MCE 9-Aminocamptothecin

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•Related Small Molecules:

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View All Topoisomerase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

9-Aminocamptothecin Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

9-Aminocamptothecin Related Classifications

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