Gimatecan
Based on 1 Customer Validation
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.28%
- No. CAS: 292618-32-7
- Fòrmula: C25H25N3O5
- Peso molecular:447.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-13670
Lurtotecan -
HY-13768A
Topotecan hydrochloride -
HY-16562
Irinotecan -
HY-13566A
Belotecan hydrochloride -
HY-16562A
Irinotecan hydrochloride -
HY-13744
Rubitecan -
HY-13758A
TAS-103 dihydrochloride -
HY-13631D
DXd -
HY-13631
Exatecan -
HY-13631A
Exatecan mesylate -
HY-13631R
Exatecan (Standard) -
HY-145397
(4-NH2)-Exatecan
Ver todos los productos específicos de isoformas Topoisomerase
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Topoisomerase I |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| carcinoma cell line | IC50 |
0.015 μM
Compound: 15
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Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)
Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)
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[PMID: 11563925] |
| HT-29 | IC50 |
0.056 μM
Compound: 2, gimatecan, GMT, ST-1481
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Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs
Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs
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[PMID: 18424133] |
| HT-29 | IC50 |
0.07 μM
Compound: 2, gimatecan, GMT, ST-1481
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Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs
Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs
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[PMID: 18424133] |
| NCI-H460 | IC50 |
0.015 μM
Compound: 2, gimatecan, GMT, ST-1481
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Antiproliferative activity against human H460 cells after 2 hrs of drug exposure measured after 72 hrs
Antiproliferative activity against human H460 cells after 2 hrs of drug exposure measured after 72 hrs
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[PMID: 18424133] |
| NCI-H460 | IC50 |
0.015 μM
Compound: 1h
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Cytotoxicity against human H460 cells
Cytotoxicity against human H460 cells
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[PMID: 18434153] |
| NCI-H460 | IC50 |
0.02 μM
Compound: 2, gimatecan, GMT, ST-1481
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Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs
Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs
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[PMID: 18424133] |
In Vitro
Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency[1].
Gimatecan causes a persistent S-phase arrest At 0.003 µg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 µg/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG)
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Concentration:3 to 300 ng/mL
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Incubation Time:1, 6, and 24 hours
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Result:IC50s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours.
IC50s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours.
The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Swiss nude mice bearing HT1376 model[1]
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Dosage:2 mg/kg
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Administration:Treatment per os, every fourth day for four times
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Result:Caused a marked tumor growth inhibition during treatment.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 292618-32-7
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Appearance Solid
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Peso molecular 447.48
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Fòrmula C25H25N3O5
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Color Light yellow to yellow
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SMILES
CC(C)(C)O/N=C/C1=C2C(C(N3C2)=CC([C@@]4(O)CC)=C(COC4=O)C3=O)=NC5=CC=CC=C15
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Synonyms
ST1481
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 6.67 mg/mL (14.91 mM; ultrasonic and warming and adjust pH to 5 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2347 mL | 11.1737 mL | 22.3474 mL | 55.8684 mL |
| 5 mM | 0.4469 mL | 2.2347 mL | 4.4695 mL | 11.1737 mL | |
| 10 mM | 0.2235 mL | 1.1174 mL | 2.2347 mL | 5.5868 mL |
Gimatecan Related Classifications
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