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BI-853520 HCl (IN10018 hydrochloride) is novel, potent and highly selective focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM) and PTK2 kinase inhibitor with anti-tumor activity.
| ln Vitro |
Ifebemtinib (BI 853520) (0-3 μM; 2 h) blocks the development of cancer cells[2]. In 3D culture alone, ifebemtinib (BI 853520) (0-30 μM; 4-6 d) suppresses the growth and invasion of tumor cells[1]. Y397-FAK autophosphorylation is suppressed by ifebemtinib (0–10 μM; 24 h)[1]. This highly metastatic murine breast cancer cell line responds quickly and potently to ifebemtinib (0.1 μM; 96 h) in terms of FAK inhibition[1].
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| ln Vivo |
Treatment with ifebemtinib (BI 853520) (oral gavage; 50 mg/kg; once daily; 0–8 weeks) dramatically inhibits the growth of all three cell lines' primary tumors in vivo[1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: PC-3 cells Tested Concentrations: 0-3 μM Incubation Duration: 2 hrs (hours) Experimental Results: Resulted in a concentration-dependent reduction of the signal with a median EC50 value of 1 nM. Cell Proliferation Assay[1] Cell Types: 4T1, Py2T, and Py2T-LT cells Tested Concentrations: 0-30 μM Incubation Duration: 4-6 days Experimental Results: Indicated that the specific inhibition of cell proliferation and invasion at low doses is functional only in three-dimensional cell culture conditions, whereas cells cultured on plastic only respond to BI 853520 at very high, toxic doses. Western Blot Analysis[1] Cell Types: 4T1, Py2T, and Py2T-LT cells Tested Concentrations: 0-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: decreased Y397-FAK autophosphorylation in all cell types. Western Blot Analysis[1] Cell Types: 4T1, Py2T, and Py2T-LT cells Tested Concentrations: 0.1 μM Incubation Duration: 96 hrs (hours) Experimental Results: diminished Y397-FAK autophosphorylation following 0.1 μM BI 853520 treatment occurred within 10 min and was substantially decreased for the fol |
| Animal Protocol |
Animal/Disease Models: FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively[1]
Doses: 50 mg/kg Route of Administration: po (oral gavage); 50 mg/kg; one time/day; 0-8 weeks Experimental Results: diminished tumor volume Dramatically over time. |
| References |
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| Molecular Formula |
C28H28F4N6O4
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|---|---|
| Molecular Weight |
588.55
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| CAS # |
1227948-82-4
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| Appearance |
White to off-white solid powder
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| SMILES |
C(NC1CCN(C)CC1)(=O)C1=CC(OC)=C(NC2=NC=C(C(F)(F)F)C(OC3=CC=CC4=C3C(=O)N(C)C4)=N2)C=C1F
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~66.67 mg/mL (~113.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6991 mL | 8.4955 mL | 16.9909 mL | |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3982 mL | |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 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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