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KIN-8194
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Catalog No. T86782Cas No. 330786-01-1
KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2].
KIN-8194
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Catalog No. T86782Cas No. 330786-01-1
KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2]. |
| In vitro | KIN-8194 (0-1 μM, 7 days) inhibits the growth of MCL cell lines (Maver-1, JeKo-1, Mino, Rec-1, and Granta-519) and primary cells [1]. It reduces proliferation in MCL cell lines by inhibiting HCK [1]. At 100 nM for 6 hours, KIN-8194 suppresses the AKT-S6 signaling pathway in Maver-1 and Granta-519 cells in an HCK-dependent manner [1]. Additionally, KIN-8194 (0-1 μM, 30 minutes) inhibits adhesion of MCL cells (JeKo-1 and Granta-519) to fibronectin or stromal cells in an HCK-dependent fashion [1]. |
| In vivo | KIN-8194, administered orally at doses ranging from 12.5 to 50 mg/kg, dose-dependently inhibits pHCK and pBTK in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse models. Additionally, a daily oral dose of 50 mg/kg over six weeks suppresses tumor growth in these models. Furthermore, a 30 mg/kg daily oral dose of KIN-8194 combined with Venetoclax extends median survival in ibrutinib-resistant BTK Cys481Ser TMD-8 cell xenograft mice [2]. |
| Molecular Weight | 483.61 |
| Formula | C28H33N7O |
| Cas No. | 330786-01-1 |
| Smiles | NC1=C2C(=NN(C2=NC=N1)[C@@H]3CC[C@H](CC3)N4CCN(C)CC4)C5=CC=C(OC6=CC=CC=C6)C=C5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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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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