| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
RIP1 kinase (IC50 = 6.3 nM)
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|---|---|
| ln Vitro |
GSK3145095 has excellent activity in blocking RIP1 kinasedependent cellular responses and potently binds to RIP1 with exquisite kinase specificity. The inhibitor is also capable of encouraging a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures, highlighting its potential as a novel cancer therapy. [1]
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| Cell Assay |
GSK3145095 is prepared in assay buffer, serially diluted 1:1.5 in a 22 point titration (high final concentration 3 μM), and added to a 384 white low volume Greiner plate. In assay buffer, 3.5 μL of each inhibitor concentration and 3.5 L of final 25 nM enzyme concentration are added to the plate. Following these additions, 3.5 μL of ATP (15.6 μM to 875 μM final) in assay buffer is added to the plate to start the reaction. At room temperature, the reaction proceeds for five hours.
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| References |
| Molecular Formula |
C20H17F2N5O2
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|---|---|
| Molecular Weight |
397.378090620041
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| Exact Mass |
397.135
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| Elemental Analysis |
C, 60.45; H, 4.31; F, 9.56; N, 17.62; O, 8.05
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| CAS # |
1622849-43-7
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| Related CAS # |
1622849-43-7
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| Appearance |
Solid powder
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| SMILES |
C1CC2=C(C(=CC(=C2)F)F)NC(=O)[C@H]1NC(=O)C3=NNC(=N3)CC4=CC=CC=C4
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| InChi Key |
ATQAGKAMBISZQM-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C20H17F2N5O2/c21-13-9-12-6-7-15(19(28)25-17(12)14(22)10-13)23-20(29)18-24-16(26-27-18)8-11-4-2-1-3-5-11/h1-5,9-10,15H,6-8H2,(H,23,29)(H,25,28)(H,24,26,27)/t15-/m0/s1
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| Chemical Name |
5-benzyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide
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| Synonyms |
GSK3145095; GSK-3145095; GSK 3145095
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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: 250~79 mg/mL (~198.8 mM)
Ethanol: ~6 mg/mL (~15.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.23 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 20.8 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: ≥ 2.08 mg/mL (5.23 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 20.8 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: ≥ 2.08 mg/mL (5.23 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 | 2.5165 mL | 12.5824 mL | 25.1648 mL | |
| 5 mM | 0.5033 mL | 2.5165 mL | 5.0330 mL | |
| 10 mM | 0.2516 mL | 1.2582 mL | 2.5165 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 |
| NCT03681951 | Terminated | Drug: GSK3145095 Drug: Pembrolizumab |
Neoplasms, Pancreatic | GlaxoSmithKline | November 16, 2018 | Phase 3 |
Products are for research use only; We do not sell to patients
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