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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Aminocamptothecin (9-amino Camptothecin, 9-AC, 9-amino CPT), an analog of camptothecin (CPT) with higher water solubility, is a potent inhibitor of topoisomerase I with anti-tumor activity. It acts by obstructing the healing process of single-strand DNA breaks. 9-AC demonstrated strong anti-proliferative activity and cytotoxicity in human HT-29 colon adenocarcinoma, with an IC50 value of 19 nM.
Targets |
Topoisomerase I
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ln Vitro |
9-Aminocamptothecin cytotoxicity rises with increasing drug concentrations and longer exposure times in human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines. Unless the concentration of 9-Aminocamptothecin surpasses a threshold of 2.7 nm, minimal cell killing is also observed[1]. After 96 hours of medication exposure, PC-3, PC-3M, DU145, and LNCaP cells are inhibited by 9-Aminocamptothecin with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively[2].
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ln Vivo |
9-Aminocamptothecin (9-Amino-CPT) suppresses tumor growth at the lowest oral dose of 0.35 mg/kg/day; tumor regression is caused by s.c. administration (4 mg/kg/week) and higher oral doses of 0.75 and 1 mg/kg/day. All dosages of 9-Aminocamptothecin are well tolerated, and no group has experienced toxic death or weight loss greater than 10%[2]. A full remission is induced in 55% of SCID mice engrafted with human myeloid leukemia by 9-Aminocamptothecin. Both the intravenous and oral routes work equally well. The evaluation of 9-Aminocamptothecin as an antileukemic agent in a phase I trial involving AML patients is supported by the results obtained from this pre-clinical model[3].
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Cell Assay |
The clonogenic assay is used to evaluate the cytotoxicity of 9-amino-CPT (9-amino-20(S)-camptothecin). 100–250 cells are inoculated in triplicate onto 60 15-mm dishes holding 5 mL of medium after exponentially growing cells are resuspended in media and the number of cells is ascertained using an electronic counter. 5 μL of 9-Aminocamptothecin stock solutions are added to the dishes to reach final concentrations of 137, 274 nM, 0.27, 1.37, 2.74, 13.7, 27.4, and 0.27 nM after an overnight incubation. Fresh medium is added to the dishes and the medium is removed by aspiration after 4, 8, 12, 24, 48, 72, and 240 hours of exposure. The ratio of colons in the drug-treated sample to those in the control (DMSO vehicle-treated) sample is used to calculate the percentage of survival at each drug concentration and exposure time[1].
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Animal Protocol |
Mice: On the seventh day following the KBM-3 cell inoculation, 9-Aminocamptothecin treatment is initiated. The following treatment is given to five groups of five mice each, with an average weight of 22 g, four days a week for three weeks: 1) PBS is IV injected into group 1 control mice; 2) group 2 mice receive 1.33 mg/kg Group 3 mice are given 1.33 mg/kg of 9-Aminocamptothecin IV. 4) Group 4 mice receive 2.0 mg/kg of 9-Aminocamptothecin IV; 5) Group 5 mice receive 2.0 mg/kg of 9-Aminocamptothecin orally by gavage. Gavage of 9-Aminocamptothecin orally[3].
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References |
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Molecular Formula |
C20H17N3O4
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Molecular Weight |
363.36668
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Exact Mass |
363.12
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Elemental Analysis |
C, 66.11; H, 4.72; N, 11.56; O, 17.61
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CAS # |
91421-43-1
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Appearance |
Solid powder
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SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC=C5N=C4C3=C2)N)O
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InChi Key |
FUXVKZWTXQUGMW-FQEVSTJZSA-N
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InChi Code |
InChI=1S/C20H17N3O4/c1-2-20(26)13-7-16-17-10(6-11-14(21)4-3-5-15(11)22-17)8-23(16)18(24)12(13)9-27-19(20)25/h3-7,26H,2,8-9,21H2,1H3/t20-/m0/s1
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Chemical Name |
(19S)-8-amino-19-ethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
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Synonyms |
9AC; 9aminoCPT; 9-amino-20-camptothecin; 9-amino-camptothecin; 9-AC9-amino-CPT; 9-amino-20(S)-camptothecin; 9aminocamptothecin; Aminocamptothecin
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~3.3 mg/mL (~9.2 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.33 mg/mL (0.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.33 mg/mL (0.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.33 mg/mL (0.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 | 0.2752 mL | 1.3760 mL | 2.7520 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00002671 | Completed | Drug: aminocamptothecin | Ovarian Cancer | Ovarian Cancer | December 1995 | Phase 2 |
NCT00002635 | Completed | Drug: aminocamptothecin Biological: filgrastim |
Lymphoma | Yale University | May 1995 | Phase 2 |
NCT00003192 | Completed | Drug: aminocamptothecin | Esophageal Cancer Gastric Cancer |
University of Chicago | March 1998 | Phase 2 |
NCT00002745 | Completed | Drug: aminocamptothecin | Lymphoma | National Cancer Institute (NCI) | April 1996 | Phase 2 |
NCT00003523 | Active Recruiting |
Drug: aminocamptothecin colloidal dispersion |
Primary Peritoneal Cavity Cancer Ovarian Cancer |
Gynecologic Oncology Group | January 1999 | Phase 2 |