Tilfrinib |
カタログ番号GC40927
One-Click Copy Product Info
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Tilfrinibは選択的なBrk/PTK6阻害剤であり、Brkに対するIC₅₀値は3.15nMである。
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は選択的なBrk/PTK6阻害剤であり、Brkに対するIC₅₀値は3.15nMである[1-2]。Tilfrinibは主に癌に関連する研究に使われている[3-4]。
In vitro（体外）実験で、ヒト肺腺癌細胞株PC9とH1975にTilfrinib（0-20μM）を24-48時間投与した。Tilfrinibは用量依存的に、PTK6タンパク質の発現を著しく阻害し、細胞の生存率を低下させた。また、TilfrinibはPC9とH1975細胞で、コロニーの形成、遊走と浸潤能力をも抑制し、アポトーシスを誘発した。Tilfrinibは、処理された細胞におけるPD-L1の発現を上方制御した[4]。ETV4 WT誘発性のUM-UC-3細胞をTilfrinib（20μM）で36時間処理した。Tilfrinibは、細胞でPTK6を阻害し、CXCL1またはCXCL8の発現を低下させた[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.
| 細胞実験[1]: | |
細胞株 | PC9とH1975細胞（ヒト肺腺癌細胞株） |
準備方法 | 37°C、5% CO₂、10%のウシ胎児血清（FBS）を添加したDMEMまたはRPMI-1640培地でPC9とH1975細胞を培養した。濃度が0–20μMのTilfrinibで細胞を24-48時間処理した。 |
反応条件 | 0–20μM；24–48時間 |
アプリケーション | Tilfrinibは用量依存的に著しく、PTK6タンパク質の発現を阻害し、細胞の生存率を低下させた。Tilfrinibは肺腺癌細胞のコロニーの形成、遊走、浸潤能力を抑制し、同時にアポトーシスを誘発した。更に、Tilfrinibの処理は、PD-L1の発現を上方制御し、潜在的な免疫調節の役割を示唆した。 |
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 |
| 溶解度 | 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.)