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

9-amino-CPT (Synonyms: 9-amino-20(S)-camptothecin)

Cat. No.: HY-100309 Purity: 98.17%
Handling Instructions

9-amino-CPT (9-amino-20(S)-camptothecin) is a topoisomerase I inhibitor with potent anticancer activity.

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

9-amino-CPT Chemical Structure

9-amino-CPT Chemical Structure

CAS No. : 91421-43-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 115 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 396 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

9-amino-CPT (9-amino-20(S)-camptothecin) is a topoisomerase I inhibitor with potent anticancer activity.

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].

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

In Vivo

9-amino-CPT (9-amino-20(S)-camptothecin) 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-amino-CPT (9-amino-20(S)-camptothecin) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group[2]. 9-amino-CPT (9-amino-20(S)-camptothecin) 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].

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

Molecular Weight

363.37

Formula

C₂₀H₁₇N₃O₄

CAS No.
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)

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 --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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

Purity: 98.89%

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Product Name:
9-amino-CPT
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HY-100309
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