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| 5mg |
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| 50mg |
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| Targets |
Tilfrinib targets breast tumor kinase (Brk/PTK6), a non-receptor tyrosine kinase involved in cell proliferation, survival, and migration. By inhibiting Brk with high potency (IC50 = 3.15 nM), Tilfrinib suppresses PTK6-dependent signaling pathways. This leads to anti-proliferative effects in breast cancer cells and other cancer types where Brk is overexpressed or activated. It is selective for Brk/PTK6 over HER2.
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| ln Vitro |
Tilfrinib (20 µM; 36 hours) decreases the production of VEGFA or MMP9 in TAN and inhibits PTK6 and ETV4 WT-induced CXCL1 or CXCL8 in UM-UC-3 cells [1]. With GI50 values of 0.99, 1.02, and 1.58 µM, tilfrinib (compound 4f) demonstrates strong anti-proliferative activity against MCF7, HS-578/T, and BT-549 cells [2].
Tilfrinib is a potent and selective Brk/PTK6 inhibitor with an IC50 of 3.15 nM. It displays good anti-proliferative activity and has anti-tumor potential. It is selective for Brk/PTK6 over HER2 (IC50 = 1,300 nM). It suppresses PTK6-dependent signaling. Its in vitro activity has been characterized in various cancer cell lines. |
| ln Vivo |
Tilfrinib has been studied in preclinical models for its anti-tumor activity. It suppresses PTK6-dependent signaling and shows anti-proliferative activity in breast cancer cell lines. It is useful for studying PTK6 kinase dependency and Brk-targeted anticancer pharmacology. Its efficacy and selectivity make it a promising tool for cancer research.
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| Enzyme Assay |
In vitro kinase assays for Tilfrinib measure its inhibition of Brk/PTK6 activity. The kinase is incubated with a substrate and ATP in the presence of varying concentrations of the compound, and phosphorylation is quantified to determine the IC50. Selectivity profiling against other kinases is performed using similar assays.
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| Cell Assay |
Western blot analysis[1]
Cell Types: UM-UC-3 cells (stably expressing FLAG-ETV4 WT or Y392F) Tested Concentrations: 20 µM Incubation Duration: 36 hrs (hours) Experimental Results: diminished CXCL1 or CXCL8 expression induced by ETV4 WT in UM-UC - Expression of VEGFA or MMP9 in 3 cells and TANs is achieved by inhibiting PTK6. In vitro cellular assays for Tilfrinib involve treating cancer cell lines with the compound and measuring cell viability, proliferation, and signaling pathway activation. Its effects on PTK6-dependent signaling are assessed by measuring phosphorylation of downstream targets. Cell cycle analysis and apoptosis detection are performed using flow cytometry. Its anti-proliferative activity is measured using MTT or similar assays. |
| Animal Protocol |
In vivo animal models for Tilfrinib include xenograft models of breast cancer and other tumors where Brk is a therapeutic target. Tumor-bearing mice are treated with the compound, and tumor growth inhibition is measured. Its effects on signaling pathways and tumor biomarkers are also assessed in these models.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Tilfrinib are limited. As a small molecule kinase inhibitor, it is expected to be absorbed after oral administration and distributed to tissues. It is metabolized in the liver, and its metabolites are excreted in urine and feces. Its half-life and bioavailability are not well-characterized in the literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of Tilfrinib is characteristic of kinase inhibitors. Its selectivity for Brk/PTK6 may reduce off-target toxicity. However, common side effects of kinase inhibitors include gastrointestinal disturbances, fatigue, and skin reactions. Its safety in humans has not been fully established.
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| References | |
| Additional Infomation |
Tilfrinib is a potent and selective inhibitor of breast tumor kinase (Brk/PTK6) with an IC50 of 3.15 nM. It displays anti-proliferative and anti-tumor activities. It is selective for Brk/PTK6 over HER2 (IC50 = 1,300 nM). It is useful for studying PTK6 kinase dependency and Brk-targeted anticancer pharmacology.
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| Molecular Formula |
C17H13N3O
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|---|---|
| Molecular Weight |
275.3046
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| Exact Mass |
275.105
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| Elemental Analysis |
C, 74.17; H, 4.76; N, 15.26; O, 5.81
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| CAS # |
1600515-49-8
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| PubChem CID |
76332983
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
560.6±35.0 °C at 760 mmHg
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| Flash Point |
292.8±25.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.839
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| LogP |
4.69
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
364
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1=C([H])C([H])=C([H])C(=C1[H])N([H])C1C([H])=C([H])N=C2C=1C1=C([H])C([H])=C([H])C([H])=C1N2[H]
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| InChi Key |
RXPZOSHFGJWSLQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13N3O/c21-12-5-3-4-11(10-12)19-15-8-9-18-17-16(15)13-6-1-2-7-14(13)20-17/h1-10,21H,(H2,18,19,20)
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| Chemical Name |
3-(9H-pyrido[2,3-b]indol-4-ylamino)phenol
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| Synonyms |
Tilfrinib;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~454.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6324 mL | 18.1620 mL | 36.3240 mL | |
| 5 mM | 0.7265 mL | 3.6324 mL | 7.2648 mL | |
| 10 mM | 0.3632 mL | 1.8162 mL | 3.6324 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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