GSK3145095
Based on 1 publication(s) in Google Scholar
GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM .
For research use only. We do not sell to patients.
- Purity: 99.39%
- CAS No.: 1622849-43-7
- Formula: C20H17F2N5O2
- Molecular Weight:397.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK3145095
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Biological Activity
IC50: 6.3 nM (RIP1 kinase )[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L929 | IC50 |
1.3 μM
Compound: 6; GSK3145095
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Inhibition of RIP1 in mouse L929 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay
Inhibition of RIP1 in mouse L929 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay
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[PMID: 31223438] |
GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1622849-43-7
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Appearance Solid
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Molecular Weight 397.38
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Formula C20H17F2N5O2
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Color White to off-white
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SMILES
FC1=CC(F)=CC2=C1NC([C@@H](NC(C3=NNC(CC4=CC=CC=C4)=N3)=O)CC2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929
Solvent & Solubility
DMSO : 250 mg/mL (629.12 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.23 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 (5.23 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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5165 mL | 12.5824 mL | 25.1648 mL | 62.9121 mL |
| 5 mM | 0.5033 mL | 2.5165 mL | 5.0330 mL | 12.5824 mL | |
| 10 mM | 0.2516 mL | 1.2582 mL | 2.5165 mL | 6.2912 mL | |
| 15 mM | 0.1678 mL | 0.8388 mL | 1.6777 mL | 4.1941 mL | |
| 20 mM | 0.1258 mL | 0.6291 mL | 1.2582 mL | 3.1456 mL | |
| 25 mM | 0.1007 mL | 0.5033 mL | 1.0066 mL | 2.5165 mL | |
| 30 mM | 0.0839 mL | 0.4194 mL | 0.8388 mL | 2.0971 mL | |
| 40 mM | 0.0629 mL | 0.3146 mL | 0.6291 mL | 1.5728 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5033 mL | 1.2582 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0485 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3146 mL | 0.7864 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6291 mL |
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