Eclitasertib
Based on 1 Customer Validation
Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of 0.0375 µΜ.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.80%
- CAS. Nr.: 2125450-76-0
- Formel: C19H18N6O3
- Molecular Weight:378.38
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Biologische Aktivität
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RIPK1 |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | CC50 |
>50 μM
Compound: 9
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Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 33930803] |
| HT-29 | EC50 |
0.0154 μM
Compound: 9
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 33930803] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mouse TNF-alpha induced hypothermia models[2]
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Dosage:
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Administration:po, single dose
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Result:Ameliorated TNF-alpha induced hypothermia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2125450-76-0
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Appearance Solid
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Molecular Weight 378.38
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Formel C19H18N6O3
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Color White to light yellow
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SMILES
O=C(C1=NN=C(CC2=CC=CC=C2)N1)N[C@@H]3C(N(C)C4=NC=CC=C4OC3)=O
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Synonyms
DNL-758; SAR-443122
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (330.36 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. 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Reinheit & Dokumentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
Verweise
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 | 2.6428 mL | 13.2142 mL | 26.4285 mL | 66.0711 mL |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2857 mL | 13.2142 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 mL | 6.6071 mL | |
| 15 mM | 0.1762 mL | 0.8809 mL | 1.7619 mL | 4.4047 mL | |
| 20 mM | 0.1321 mL | 0.6607 mL | 1.3214 mL | 3.3036 mL | |
| 25 mM | 0.1057 mL | 0.5286 mL | 1.0571 mL | 2.6428 mL | |
| 30 mM | 0.0881 mL | 0.4405 mL | 0.8809 mL | 2.2024 mL | |
| 40 mM | 0.0661 mL | 0.3304 mL | 0.6607 mL | 1.6518 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5286 mL | 1.3214 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4405 mL | 1.1012 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8259 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6607 mL |
Eclitasertib Related Classifications
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