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Chemical Structure| 1227948-82-4 Chemical Structure| 1227948-82-4

Structure of Ifebemtinib
CAS No.: 1227948-82-4

Chemical Structure| 1227948-82-4

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Ifebemtinib (BI 853520)is an orally active Focal Adhesion Kinase (FAK) inhibitor with anti-proliferative activity against cancer cells.

Synonyms: IN-10018; BI-853520

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Product Details of Ifebemtinib

CAS No. :1227948-82-4
Formula : C28H28F4N6O4
M.W : 588.55
SMILES Code : O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(C(F)(F)F)C(OC4=CC=CC(CN5C)=C4C5=O)=N3)C=C2F
Synonyms :
IN-10018; BI-853520
MDL No. :MFCD34676862

Safety of Ifebemtinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Ifebemtinib

RTK
cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC-3 prostate carcinoma cells 3 nmol/L blocks anchorage-independent proliferation Oncogenesis. 2018 Feb 23;7(2):21
SPC111, SPC212, P31, and M38K cells 0.1 μM and 1 μM 96 hours To assess the effect of BI 853520 on spheroid formation, BI 853520 significantly reduced spheroid numbers J Mol Med (Berl). 2019 Feb;97(2):231-242
SPC111, SPC212, P31, and M38K cells 1 μM 24 hours To evaluate the effect of BI 853520 on cell migration, BI 853520 showed anti-migratory effects in three out of four cell lines J Mol Med (Berl). 2019 Feb;97(2):231-242
Py2T-LT cells 1 µM 24 hours BI 853520 significantly reduces Y397-FAK autophosphorylation. Oncogenesis. 2018 Sep 20;7(9):73
Py2T cells 1 µM 24 hours BI 853520 significantly reduces Y397-FAK autophosphorylation. Oncogenesis. 2018 Sep 20;7(9):73
4T1 cells 0.1 µM 24 hours BI 853520 significantly reduces Y397-FAK autophosphorylation. Oncogenesis. 2018 Sep 20;7(9):73
Calu-6 lung adenocarcinoma cells 3 nmol/L inhibition of cell proliferation Oncogenesis. 2018 Feb 23;7(2):21

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Breast cancer models Oral 50 mg/kg Once daily for 8 weeks BI 853520 significantly suppresses primary tumor growth and tumor progression. Oncogenesis. 2018 Sep 20;7(9):73
Nude mice PC-3 prostate adenocarcinoma xenografts Oral 50 mg/kg Once daily for 17 days Inhibition of tumor growth Oncogenesis. 2018 Feb 23;7(2):21
SCID mice Orthotopic MPM xenograft model Oral 20 mg/kg Five times a week for 3 weeks To evaluate the effect of BI 853520 on tumor growth, BI 853520 significantly reduced tumor load, tumor cell proliferation, and microvessel density J Mol Med (Berl). 2019 Feb;97(2):231-242

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.50mL

1.70mL

0.85mL

16.99mL

3.40mL

1.70mL

 

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