Tilfrinib |
Catalog No.GC40927
One-Click Copy Product Info
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Tilfrinib is a selective Brk/PTK6 inhibitor with an IC₅₀ value of 3.15nM for Brk.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1600515-49-8
Sample solution is provided at 25 µL, 10mM.
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Tilfrinib is a selective Brk/PTK6 inhibitor with an IC₅₀ value of 3.15nM for Brk[1-2]. Tilfrinib is primarily used in cancer-related research[3-4].
In vitro, Tilfrinib (0-20μM) was administered to human lung adenocarcinoma cell lines PC9 and H1975 for 24-48 hours. Tilfrinib significantly inhibited PTK6 protein expression and reduced cell viability in a dose-dependent manner. Tilfrinib also suppressed colony formation, migration, and invasion capabilities in PC9 and H1975 cells, and induced apoptosis. Tilfrinib upregulated PD-L1 expression in the treated cells[4]. ETV4 WT-induced UM-UC-3 cells were treated with Tilfrinib (20μM) for 36 hours. Tilfrinib inhibited PTK6 and reduced the expression of CXCL1 or CXCL8 in cells[5].
References:
[1] Mahmoud KA, Krug M, Wersig T, et al. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1948-51.
[2] Chen B, Liu B, Chen J, et al. PTK6 drives HNRNPH1 phase separation to activate autophagy and suppress apoptosis in colorectal cancer. Autophagy. 2025 Aug;21(8):1680-1699.
[3] Jerin S, Harvey AJ, Lewis A. Therapeutic Potential of Protein Tyrosine Kinase 6 in Colorectal Cancer. Cancers (Basel). 2023 Jul 21;15(14):3703.
[4] Xiong RH, Yang SQ, Li JW, et al. Identification of immune-associated biomarker for predicting lung adenocarcinoma: bioinformatics analysis and experiment verification of PTK6. Discov Oncol. 2024 Apr 4;15(1):102.
[5] Zhang Q, Liu S, Wang H, et al. ETV4 Mediated Tumor-Associated Neutrophil Infiltration Facilitates Lymphangiogenesis and Lymphatic Metastasis of Bladder Cancer. Adv Sci (Weinh). 2023 Apr;10(11):e2205613.
| Cell experiment [1]: | |
Cell lines | PC9 and H1975 cells (human lung adenocarcinoma cell lines) |
Preparation Method | PC9 and H1975 cells were maintained in DMEM or RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Tilfrinib at concentrations of 0–20μM for 24–48 hours. |
Reaction Conditions | 0–20μM; 24–48h. |
Applications | Tilfrinib significantly inhibited PTK6 protein expression and reduced cell viability in a dose-dependent manner. Tilfrinib suppressed colony formation, migration, and invasion capabilities of lung adenocarcinoma cells, while inducing apoptosis. Additionally, Tilfrinib treatment upregulated PD-L1 expression, suggesting a potential immunomodulatory role. |
References: | |
| Cas No. | 1600515-49-8 | SDF | |
| Canonical SMILES | OC1=CC=CC(NC2=CC=NC3=C2C4=C(C=CC=C4)N3)=C1 | ||
| Formula | C17H13N3O | M.Wt | 275.3 |
| Solubility | DMSO: 23 mg/ml,Ethanol: 13 mg/ml | Storage | Store at -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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6324 mL | 18.162 mL | 36.324 mL |
| 5 mM | 726.5 μL | 3.6324 mL | 7.2648 mL |
| 10 mM | 363.2 μL | 1.8162 mL | 3.6324 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)