PROTAC FAK degrader 5
PROTAC FAK degrader 5 is a potent PROTAC degrader targeting FAK, with a DC50 of 11.65 nM. PROTAC FAK degrader 5 induces FAK protein degradation, selectively inhibits colony formation of human colorectal cancer HCT116 cells, and blocks the proliferation of human umbilical vein endothelial HUVEC cells, exhibiting anti-angiogenic activity. PROTAC FAK degrader 5 can be used in the research of colorectal cancer and angiogenesis.
(Pink: FAK ligand (HY-183769); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Formula: C40H37F3N10O7
- Molecular Weight:826.78
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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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Biological Activity
PROTAC FAK degrader 5 (compound 16g) (72 h) potently inhibits HCT116 colorectal cancer cell proliferation with an IC50 of 1.56 μM and exhibits no cytotoxicity toward normal L02 cells[1].
PROTAC FAK degrader 5 (0.020-20 μM; 0.5-72 h) potently degrades FAK protein in HCT116 colorectal cancer cells with a DC50 of 11.65 nM[1].
PROTAC FAK degrader 5 (0.32-20 μM; 72 h) induces dose-dependent cytotoxic morphological changes in HCT116 colorectal cancer cells[1].
PROTAC FAK degrader 5 (0.31-10 μM; 48 h) induces dose-dependent cytotoxicity in HCT116 colorectal cancer cells[1].
PROTAC FAK degrader 5 (0.25-2 μM; 10 days) potently and dose-dependently suppresses long-term clonogenic survival of HCT116 colorectal cancer cells[1].
PROTAC FAK degrader 5 (72 h) inhibits human umbilical vein endothelial HUVEC cell proliferation with an IC50 of 23.37 μM, demonstrating anti-angiogenic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colorectal cancer HCT116 cells
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Concentration:0.02, 0.039, 0.078, 0.16, 0.3, 0.63, 1.25, 2.5, 5, 10, 20 μM (24 h incubation); 5 μM (time-course incubation)
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Incubation Time:0.5, 1, 2, 4, 6, 12, 24, 48, 72 h (5 μM concentration); 24 h (0.020-20 μM concentrations)
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Result:Induced approximately 80% or greater FAK degradation at 0.63 μM (24 h incubation).
Showed a DC50 (half-maximal degradation concentration) of 11.65 nM.
Induced obvious FAK degradation as early as 2 h of treatment with 5 μM, and almost complete degradation by 6 h.
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Cell Line:human colorectal cancer HCT116 cells
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Concentration:0.25, 0.5, 1, 2 μM
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Incubation Time:10 days
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Result:Induced potent, dose-dependent suppression of colony formation.
A significant reduction in colony number and size was observed at 0.25 μM, and clonogenic survival was markedly impaired compared to the positive control.
| Species | Dose | Route | C0 | CL | Vss | T1/2 | AUClast | AUCinf | MRT0-inf |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 1891 ng/mL | 138.0 mL/min/kg | 6.52 L/kg | 2.01 h | 242 ng·h/mL | 246 ng·h/mL | 0.80 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 826.78
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Formula C40H37F3N10O7
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SMILES
O=C(NCC1=CN=NN1CCCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)C5=CC=C(NC6=NC=C(C(F)(F)F)C(OC7=CC=CC=C7OC)=N6)C=C5
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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 5 Related Classifications
HY-183768 Related Classifications
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