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).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2471525-44-5
- 分子式: C41H43ClN10O7
- 分子量:823.30
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
IC50: 14.9 nM (FAK)[1]
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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] |
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.
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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).
化学情報
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CAS 番号 2471525-44-5
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分子量 823.30
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FAK PROTAC B5 関連分類
HY-143458 関連分類
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