Ifebemtinib
Ifebemtinib Basic information
- Product Name:
- Ifebemtinib
- Synonyms:
-
- Benzamide, 4-[[4-[(2,3-dihydro-2-methyl-3-oxo-1H-isoindol-4-yl)oxy]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)-
- IN10018（BI853520）
- IN10018
- Ifebemtinib (BI-853520)
- Ifebemtinib
- Ifebemtinib/BI-853520/IN-10018
- 2-Fluoro-5-methoxy-4-[[4-[(2-methyl-3-oxo-4-isoindolinyl)oxy]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-N-(1-methyl-4-piperidyl)benzamide
- 2-Fluoro-5-methoxy-4-((4-((2-methyl-3-oxoisoindolin-4-yl)oxy)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-N-(1-methylpiperidin-4-yl)benzamide , Ifebemtinib
- CAS:
- 1227948-82-4
- MF:
- C28H28F4N6O4
- MW:
- 588.55
- Mol File:
- 1227948-82-4.mol
Ifebemtinib Chemical Properties
- Density
- 1.45±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 13.19±0.20(Predicted)
- form
- Solid
- color
- White to off-white
- InChIKey
- ULMMVBPTWVRPSI-UHFFFAOYSA-N
- 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
Ifebemtinib Usage And Synthesis
Uses
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively[1][2][3].
in vivo
Ifebemtinib (BI 853520) (oral gavage; 50 mg/kg; once daily; 0-8 weeks) treatment significantly suppresses primary tumor growth of all three cell lines in vivo[1].
| Animal Model: | FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; 50 mg/kg; once daily; 0-8 weeks |
| Result: | Decreased tumor volume significantly over time. |
References
[1] Hirt UA, et al. Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype. Oncogenesis. 2018 Feb 23;7(2):21. DOI:10.1038/s41389-018-0032-z
[2] Stefanie Tiede, et al. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis. 2018 Sep 20;7(9):73. DOI:10.1038/s41389-018-0083-1
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