PROTAC FAK degrader 3
PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers.
(Pink: FAK ligand (HY-143407); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Formula: C48H50N8O9
- Molecular Weight:882.96
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Storage:
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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Biological Activity
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Chemical Information
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- References
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Biological Activity
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Cereblon |
PROTAC FAK degrader 3 (Compound D4) (0-1000 nM, 24 h) induces FAK degradation in PA-1, ID8, 4T1, H22, HEY, MDA-MB-231, and PLC/PRF5 cells, induces 89% degradation of FAK at 50 nM and 92% degradation of FAK at 500 nM in PA-1 cells [1].
PROTAC FAK degrader 3 (1 μM) inhibits FAK (99%) (IC50 = 0.44 nM), STK33 (92%), CLK4 (87%), and Fes (86%) kinase activity[1].
PROTAC FAK degrader 3 (0.01-100 μM, 72 h) exhibits antiproliferative activity against PA-1, HEY, and Huh-7 cells[1].
PROTAC FAK degrader 3 (0-3 μM, 1-7 days) reduces colony formation, migration, and invasion in PA-1 cells[1].
PROTAC FAK degrader 3 (3 μM, 24 h) upregulates genes related to tumor immunogenicity, antigen presentation-related genes (HLA-B, HLA-F, and B2M), and immunoproteasome-related genes (PSMB8 and PSMB9) in PA-1 cells[1].
PROTAC FAK degrader 3 (3 μM, 24 h) promotes antigen presentation and MHC-I expression on the surface of tumor cells in ID8, PA-1, H22, PLC/PRF5 cells[1].
PROTAC FAK degrader 3 (3 μM, 72 h) promotes the activation and proliferation of antigen-specific CD8 T cells in ID8 cells cocultured with activated murine CD8 T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PA-1 cells
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Concentration:0 nM, 0.14 nM, 0.41 nM, 1.23 nM, 3.7 nM, 11.1 nM, 33.3 nM, 100 nM
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Incubation Time:0 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
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Result:Induced FAK degradation, with almost complete degradation at 11.1 nM and achieved almost complete degradation at 24 h.
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Cell Line:ID8, 4T1, H22, HEY, MDA-MB-231, and PLC/PRF5 cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced FAK degradation.
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Cell Line:PA-1, H22 cells
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Concentration:3, 10, 30 nM
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Incubation Time:24 h
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Result:Induced FAK degradation, showed comparable degradation activity to GSK215 (HY-132296) and was more effective than BI-3663 (HY-111546).
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Cell Line:PA-1 cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Had little effect on FAK mRNA levels.
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Cell Line:PA-1 cells
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Reduced migration and invasion ability.
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Cell Line:ID8, PA-1, H22, PLC/PRF5 cells
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Concentration:3 μM
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Incubation Time:72 h
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Result:Induced FAK degradation.
| Species | Dose | Route | Cmax |
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| Mice[1] | 15 mg/kg | i.p. | 94.93 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:H22 (1 × 106) tumor-bearing syngeneic mice (6 week-old BALB/cJ) model[1]
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Dosage:15 mg/kg
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Administration:i.p., once a day, 8 days
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Result:Inhibited tumor growth without affecting the body weight, enhanced expression of H2-Kd/H2-Dd on CD45- tumor cells (3.19-fold versus vehicle), without affecting Pd-l1 expression, expressed a higher level of CD107a (2.82-fold versus vehicle), indicating enhanced cell cytotoxicity.
Chemical Information
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Molecular Weight 882.96
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Formula C48H50N8O9
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SMILES
O=C1CCC2=C1C(OC3=NC(NC4=CC=C(C=C4OC)C(NC5CCN(CC5)CCCCCCCOC6=C7C(C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=CC=C6)=O)=NC9=C3C=CN9)=CC=C2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC FAK degrader 3 Related Classifications
HY-175459 Related Classifications
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