1. Protein Tyrosine Kinase/RTK PROTAC
  2. FAK PROTACs
  3. FAK PROTAC B5

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion.

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FAK PROTAC B5

FAK PROTAC B5 Estructura química

No. CAS : 2471525-44-5

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Descripciòn

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

IC50 & Target

IC50: 14.9 nM (FAK)[1]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.14 μM
Compound: B5
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35486993]
In Vitro

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1].
FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1].
FAK PROTAC B5 exhibits a moderate membrane permeability[1].

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

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 8 h
Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM).

Cell Invasion Assay[1]

Cell Line: A549
Concentration: 0.20, 0.60 and 1.80 μM
Incubation Time: 72 h
Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.
In Vivo

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

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

Peso molecular

823.30

Fòrmula

C41H43ClN10O7

No. CAS
SMILES

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCN4CCN(C5=CC=C(NC6=NC=C(Cl)C(NC7=CC=CC=C7C(NC)=O)=N6)C(OC)=C5)CC4

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

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Referencias
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  • 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.

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Inquiry Information

Nombre del producto:
FAK PROTAC B5
Cat. No.:
HY-143458
Cantidad:
MCE Japan Authorized Agent: