KIN-8194 |
| رقم الكتالوجGC73775 |
KIN-8194 هو مثبط ثنائي نشط عن طريق الفم من HCK و BTK، مع قيم IC50 من 0.915 و <0.495 نانومتر، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 330786-01-1
Sample solution is provided at 25 µL, 10mM.
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KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice.
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].KIN-8194 (0-1 μM, 7 days) reduces MCL cell lines proliferation through HCK inhibition[1].KIN-8194 (100 nM, 6 h) inhibits the AKT-S6 signaling pathway in Maver-1 and Granta-519 cells in an HCK-dependent manner[1].KIN-8194 (0-1 μM, 30 min) inhibits adhesion of MCL cells ( JeKo-1 and Granta-519) to fibronectin or stromal cells in an HCK-dependent manner[1].
KIN-8194 (12.5-50 mg/kg, p.o., once time) blocks pHCK and pBTK in a dose-dependent manner in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model[2].KIN-8194 (50 mg/kg, p.o., daily, 6 weeks) inhibits tumor growth in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model[2].KIN-8194 (30 mg/kg, p.o., daily, 22 days) combined with Venetoclax prolongs the survival of ibrutinib-resistant BTKCys481Ser TMD-8 cells xenograft mice median survival time[2].
References:
[1]. Lantermans HC, et al. The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma. Leukemia. 2024 Mar 7.
[2]. Yang G, et al. The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. 2021 Nov 18;138(20):1966-1979.
| Cas No. | 330786-01-1 | SDF | |
| Formula | C28H33N7O | M.Wt | 483.61 |
| الذوبان | Storage | -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0678 mL | 10.3389 mL | 20.6778 mL |
| 5 mM | 0.4136 mL | 2.0678 mL | 4.1356 mL |
| 10 mM | 0.2068 mL | 1.0339 mL | 2.0678 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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