Gemcitabine elaidate hydrochloride
Based on 5 publication(s) in Google Scholar
Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.
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- Pureza : 97.39%
- No. CAS: 2918768-08-6
- Fòrmula: C27H44ClF2N3O5
- Peso molecular:564.11
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
Publications Citing Use of MedChemExpress (MCE) Gemcitabine elaidate hydrochloride
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Actividad biológica
Descripciòn
In Vitro
Gemcitabine elaidate (0.2 nM-1 mM; 72 h) hydrochloride inhibits the growth of gemcitabine sensitive and resistant cells, with IC50s of 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4 and MOLT4/C8 cells, respectively[1].
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Gemcitabine elaidate (0.5 nM-1 μM; 72 h) hydrochloride increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and WiDR cells
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Concentration:0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM
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Incubation Time:72 h
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Result:Induced a G2/M and S phase accumulation.
In Vivo
? Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) hydrochloride shows acceptable toxicity and significant antitumor activity in the colon cancer xenograft Co6044 bearing mice[1].
? Gemcitabine elaidate (p.o. once daily for 5 doses) hydrochloride shows a favorable toxicity and antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively[1]
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Dosage:25-120 mg/kg
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Administration:I.p. every 3 days for 5 doses
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Result:Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2918768-08-6
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Appearance Solid
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Peso molecular 564.11
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Fòrmula C27H44ClF2N3O5
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Color White to off-white
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SMILES
O[C@@H](C(F)(F)[C@H](N1C(N=C(C=C1)N)=O)O2)[C@H]2COC(CCCCCCC/C=C/CCCCCCCC)=O.[H]Cl
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Synonyms
CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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J Nanobiotechnology
A mucoadhesive-to-penetrating nanomotors-in-hydrogel system for urothelium-oriented intravesical drug delivery. [Abstract]2024 Sep 14;22(1):560. PMID: 39272197 -
J Control Release
R11 modified tumor cell membrane nanovesicle-camouflaged nanoparticles with enhanced targeting and mucus-penetrating efficiency for intravesical chemotherapy for bladder cancer. [Abstract]2022 Nov:351:834-846. PMID: 36191674 -
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
ACS Infect Dis
Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]2025 Oct 30. PMID: 41166549
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (177.27 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bergman AM, et, al. Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models. Invest New Drugs. 2011 Jun;29(3):456-66. [Content Brief]
[2]. Adema AD, et, al. Cell cycle effects of fatty acid derivatives of cytarabine, CP-4055, and of gemcitabine, CP-4126, as basis for the interaction with oxaliplatin and docetaxel. Int J Oncol. 2010 Jan;36(1):285-94. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.7727 mL | 8.8635 mL | 17.7270 mL | 44.3176 mL |
| 5 mM | 0.3545 mL | 1.7727 mL | 3.5454 mL | 8.8635 mL | |
| 10 mM | 0.1773 mL | 0.8864 mL | 1.7727 mL | 4.4318 mL | |
| 15 mM | 0.1182 mL | 0.5909 mL | 1.1818 mL | 2.9545 mL | |
| 20 mM | 0.0886 mL | 0.4432 mL | 0.8864 mL | 2.2159 mL | |
| 25 mM | 0.0709 mL | 0.3545 mL | 0.7091 mL | 1.7727 mL | |
| 30 mM | 0.0591 mL | 0.2955 mL | 0.5909 mL | 1.4773 mL | |
| 40 mM | 0.0443 mL | 0.2216 mL | 0.4432 mL | 1.1079 mL | |
| 50 mM | 0.0355 mL | 0.1773 mL | 0.3545 mL | 0.8864 mL | |
| 60 mM | 0.0295 mL | 0.1477 mL | 0.2955 mL | 0.7386 mL | |
| 80 mM | 0.0222 mL | 0.1108 mL | 0.2216 mL | 0.5540 mL | |
| 100 mM | 0.0177 mL | 0.0886 mL | 0.1773 mL | 0.4432 mL |
Gemcitabine elaidate hydrochloride Related Classifications
HY-13538A Related Classifications
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