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Ifebemtinib

Catalog No. T64167 CAS 1227948-82-4

Synonyms: IN-10018, BI-853520

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.

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Ifebemtinib, CAS 1227948-82-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 165.00
5 mg	In stock	$ 413.00
10 mg	In stock	$ 689.00
25 mg	In stock	$ 1,490.00

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Purity: 99.82%

Purity: 98.33%

Purity: 98.07%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.
Targets&IC50	FAK:1 nM, FER:900 nM, FES:1040 nM
In vitro	4T1, Py2T, and Py2T-LT cells were exposed to increasing concentrations of BI-853520 (0, 0.1, 0.5, 1, 5, and 10 μM for 4T1 cells; 1, 3, and 10 μM for Py2T and Py2T-LT cells) for 24 hours. The results demonstrate that BI-853520 reduces Y397-FAK phosphorylation in a dose-dependent and time-dependent manner[2].
In vivo	In PC-3 cells, BI-853520（Ifebemtinib；0-3 μM; 2 h) resulted in a concentration-dependent reduction of the signal, with a median EC50 value of 1 nM[2].

Synonyms	IN-10018, BI-853520
Molecular Weight	588.55
Formula	C28H28F4N6O4
CAS No.	1227948-82-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (84.89 mM)

References and Literature

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. 2. Stefanie Tiede, et al. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis. 2018 Sep 20;7(9):73. 3. Ulrich A Hirt, 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.

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Keywords

Ifebemtinib 1227948-82-4 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK IN-10018 BI-853520 inhibitor inhibit

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