2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. Ifebemtinib

Ifebemtinib  (Synonyms: BI-853520; IN-10018)

Cat. No.: HY-122844 Purity: 99.86%
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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.

For research use only. We do not sell to patients.

Ifebemtinib Chemical Structure

Ifebemtinib Chemical Structure

CAS No. : 1227948-82-4

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50 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

Ifebemtinib Related Antibodies

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  • Purity & Documentation

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Description

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].

IC50 & Target

IC50: 1  nM (recombinant FAK)[1], 900 nM (FER Kinase), 1040 nM (FES Kinase)[3]
In Vitro

Ifebemtinib (BI 853520) (0-3 μM; 2 h) inhibits cancer cells growth[2].
Ifebemtinib (BI 853520) (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture[1].
Ifebemtinib (0-10 μM; 24 h) represses Y397-FAK autophosphorylation[1].
Ifebemtinib (0.1 μM; 96 h) shows a fast and potent inhibition of FAK in this highly metastatic murine breast cancer cell line[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ifebemtinib Related Antibodies

Cell Viability Assay[2]

Cell Line: PC-3 cells
Concentration: 0-3 μM
Incubation Time: 2 hours
Result: Resulted in a concentration-dependent reduction of the signal with a median EC50 value of 1 nM.

Cell Proliferation Assay[1]

Cell Line: 4T1, Py2T, and Py2T-LT cells
Concentration: 0-30 μM
Incubation Time: 4-6 days
Result: 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 Line: 4T1, Py2T, and Py2T-LT cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Reduced Y397-FAK autophosphorylation in all cell types.

Western Blot Analysis[1]

Cell Line: 4T1, Py2T, and Py2T-LT cells
Concentration: 0.1 μM
Incubation Time: 96 hours
Result: Decreased Y397-FAK autophosphorylation following 0.1 µM BI 853520 treatment occurred within 10 min and was substantially reduced at least for the following 48 h.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

588.55

Formula

C28H28F4N6O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(F)C=C(NC2=NC=C(C(F)(F)F)C(OC3=CC=CC4=C3C(N(C4)C)=O)=N2)C(OC)=C1)NC5CCN(CC5)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (101.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1 mg/mL (1.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.86%

COA (249 KB) HNMR (183 KB) RP-HPLC (206 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6991 mL 8.4955 mL 16.9909 mL 42.4773 mL
5 mM 0.3398 mL 1.6991 mL 3.3982 mL 8.4955 mL
10 mM 0.1699 mL 0.8495 mL 1.6991 mL 4.2477 mL
15 mM 0.1133 mL 0.5664 mL 1.1327 mL 2.8318 mL
20 mM 0.0850 mL 0.4248 mL 0.8495 mL 2.1239 mL
25 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6991 mL
30 mM 0.0566 mL 0.2832 mL 0.5664 mL 1.4159 mL
40 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0619 mL
50 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8495 mL
60 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7080 mL
80 mM 0.0212 mL 0.1062 mL 0.2124 mL 0.5310 mL
100 mM 0.0170 mL 0.0850 mL 0.1699 mL 0.4248 mL
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Ifebemtinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ifebemtinib1227948-82-4BI-853520 IN-10018BI853520BI 853520IN10018IN 10018IN-10018FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseanti-proliferative activityoral activityPC-34T1Py2TPy2T-LTInhibitorinhibitorinhibit

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