2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. 9-Aminocamptothecin

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

製品番号: HY-100309 純度: 98.80%
COA 取扱説明書 Technical Support

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

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9-Aminocamptothecin

9-Aminocamptothecin 構造式

CAS 番号 : 91421-43-1

容量 価格（税別） 在庫状況 数量
2 mg $64 在庫あり
5 mg $115 在庫あり
10 mg $180 在庫あり
25 mg $320 在庫あり
50 mg $470 在庫あり
100 mg $680 在庫あり
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Based on 1 publication(s) in Google Scholar

9-Aminocamptothecin 関連抗体

Top Publications Citing Use of Products

Topoisomerase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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]
COLO 205 IC50
6.6 nM
Compound: 5
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human colorectal cells (COLO 205)
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human colorectal cells (COLO 205)
[PMID: 10479293]
HepG2 IC50
3.5 nM
Compound: 5
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human hepatocellular cells (HepG2)
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human hepatocellular cells (HepG2)
[PMID: 10479293]
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]
HT-29 IC50
7.4 nM
Compound: 5
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human colorectal cells (HT-29)
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]thymidine into cellular DNA of human colorectal cells (HT-29)
[PMID: 10479293]
KB ED50
0.02 μg/mL
Compound: 4
In vitro cytotoxic activity against KB cell culture.
In vitro cytotoxic activity against KB cell culture.
[PMID: 3656353]
L1210 IC50
12 nM
Compound: 27
Inhibitory activity in mice bearing L1210 leukemia
Inhibitory activity in mice bearing L1210 leukemia
[PMID: 1846923]
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
L1210 IC50
12.7 nM
Compound: 2 (9-AC, 9-Amino Camptothecin)
Compound was tested in vitro for cytotoxicity against L1210 murine leukemia cells.
Compound was tested in vitro for cytotoxicity against L1210 murine leukemia cells.
10.1016/0960-894X(96)00083-2
NCI-H928 IC50
7.9 nM
Compound: 5
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]-thymidine into cellular DNA of human lung carcinoma cells (H928)
Cytotoxicity expressed as the concentration that inhibited incorporation of [3H]-thymidine into cellular DNA of human lung carcinoma cells (H928)
[PMID: 10479293]
体外実験

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.

9-Aminocamptothecin 関連抗体
体内実験

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.
臨床実験
分子量

363.37

分子式

C20H17N3O4
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
純度とドキュメンテーション

純度: 98.89%

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

取扱説明書 (2659 KB)
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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