| Identification | Back Directory | [Name]
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)- | [CAS]
1227948-82-4 | [Synonyms]
IN10018
IN10018（BI853520）
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)- | [Molecular Formula]
C28H28F4N6O4 | [MOL File]
1227948-82-4.mol | [Molecular Weight]
588.55 |
| Chemical Properties | Back Directory | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
13.19±0.20(Predicted) | [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 |
| Hazard Information | Back Directory | [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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