FAK PROTAC B5
FAK PROTAC B5 is a FAK PROTAC degrader with an IC50 of 14.9 nM. FAK PROTAC B5 induces FAK degradation via the ubiquitin-proteasome pathway by simultaneously binding to FAK and the CRBN E3 ligase. FAK PROTAC B5 inhibits the proliferation, migration and invasion of cancer cells. FAK PROTAC B5 can be used for the research of non-small cell lung cancer.
(Pink: EGFR Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2471525-44-5
- Formula: C41H43ClN10O7
- Molecular Weight:823.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
IC50: 14.9 nM (FAK)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.14 μM
Compound: B5
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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
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[PMID: 35486993] |
In Vitro
FAK PROTAC B5 (compound B5) potently inhibits the activity of purified FAK kinase with an IC50 of 14.9 nM; it also potently inhibits the proliferation of A549 cells, with an IC50 of 0.14 μM after 72 h of treatment[1].
FAK PROTAC B5 (2.00 μM; 2 h) exhibits moderate membrane permeability in Caco-2 cell monolayers, with a Papp value of 1.4 × 10-6 cm/s in the A-to-B direction[1].
FAK PROTAC B5 (0.01-1 μM; 12 h) degrades 86.4% of FAK protein in A549 cells; this degradation process requires binding to FAK, interaction with the CRBN E3 ligase, and proceeds via the proteasomal pathway[1].
FAK PROTAC B5 (0.20-1.80 μM; 72 h) inhibits migration and invasion of A549 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A549 non-small cell lung cancer cells
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Concentration:0.01, 0.1, 1 μM
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Incubation Time:12 h
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Result:Induced 86.4% degradation of FAK protein after 12 h of treatment.
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Cell Line:A549 non-small cell lung cancer cells
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Concentration:10 nM (FAK PROTAC B5)
5 μM TAE-226, 5 μM Pomalidomide, 5 μM MG-132 (pretreatment) -
Incubation Time:12 h (FAK PROTAC B5 treatment); 2 h (pretreatment)
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Result:Almost completely prevented FAK degradation by FAK PROTAC B5 when cells were pretreated with TAE-226 (HY-13203), Pomalidomide (HY-10984), or MG-132 (HY-13259).
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Cell Line:A549 non-small cell lung cancer cells
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Concentration:0.20 μM, 0.60 μM, 1.80 μM
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Incubation Time:72 h
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Result:Inhibited A549 cell migration in a concentration-dependent manner.
Reduced 72 h wound recovery to 42.2% at 0.20 μM.
Reduced 72 h wound recovery to 33.3% at 0.60 μM.
Reduced 72 h wound recovery to 21.7% at 1.80 μM.
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Cell Line:A549 non-small cell lung cancer cells
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Concentration:0.20 μM, 0.60 μM, 1.80 μM
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Incubation Time:72 h
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Result:Inhibited A549 cell invasion in a concentration-dependent manner.
Reduced the number of invasive cells.
Exhibited activity superior to TAE-226 (HY-13203).
Chemical Information
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CAS No. 2471525-44-5
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Molecular Weight 823.30
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Formula C41H43ClN10O7
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)