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Tilpisertib
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Catalog No. T39466Cas No. 2065153-41-3
Alias GS-4875, GS4875, GS 4875
Tilpisertib is a serine/threonine kinase inhibitor disclosed in patent WO2017007689, designed to modulate aberrant kinase-driven signaling pathways, and is used extensively in cancer biology and signal transduction research to investigate kinase-dependent cell proliferation, survival, and resistance mechanisms, supporting preclinical evaluation of targeted therapeutic strategies.
Tilpisertib
😃Good
Catalog No. T39466Alias GS-4875, GS4875, GS 4875Cas No. 2065153-41-3
Tilpisertib is a serine/threonine kinase inhibitor disclosed in patent WO2017007689, designed to modulate aberrant kinase-driven signaling pathways, and is used extensively in cancer biology and signal transduction research to investigate kinase-dependent cell proliferation, survival, and resistance mechanisms, supporting preclinical evaluation of targeted therapeutic strategies.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $970 | 7-10 days | 7-10 days |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | Tilpisertib is a serine/threonine kinase inhibitor disclosed in patent WO2017007689, designed to modulate aberrant kinase-driven signaling pathways, and is used extensively in cancer biology and signal transduction research to investigate kinase-dependent cell proliferation, survival, and resistance mechanisms, supporting preclinical evaluation of targeted therapeutic strategies. |
| In vitro | In enzymatic assays, Tilpisertib inhibited TPL2 kinase activity with an IC50 of 1.3 nM, showing selectivity against other MAPKs. In primary human monocytes and dendritic cells stimulated by LPS or TNF-α, treatment with the compound blocked the TPL2-MEK-ERK axis and suppressed the secretion of pro-inflammatory cytokines including TNF-α, IL-1β, IL-6, and IL-8 [1]. |
| In vivo | In a rat model of acute inflammation induced by LPS, oral administration of Tilpisertib reduced serum TNF-α levels with an EC50 of 667 nM. In preclinical models of colitis, inhibition of TPL2 by the compound was associated with reduced tissue pERK levels and a lower inflammatory cytokine burden, leading to an amelioration of disease pathology in the colon [1]. |
| Synonyms | GS-4875, GS4875, GS 4875 |
| Molecular Weight | 593.13 |
| Formula | C33H33ClN8O |
| Cas No. | 2065153-41-3 |
| Smiles | [C@@H](NC1=CC=2C(NCC(C)(C)C)=C(C#N)C=NC2C(Cl)=C1)(C3=CN(C45CC(C4)C5)N=N3)C6=C7C(C(=O)N(C)C=C7)=CC=C6 |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (168.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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