PROTAC FAK degrader 4
PROTAC FAK degrader 4 is a potent FAK PROTAC degrader with a DC50 of 3.6 nM. PROTAC FAK degrader 4 induces FAK ubiquitination and degradation via the VHL-dependent ubiquitin-proteasome pathway. PROTAC FAK degrader 4 inhibits cell proliferation, colony formation, migration and invasion. Combination of PROTAC FAK degrader 4 with Cisplatin (HY-17394) enhances chemosensitivity. PROTAC FAK degrader 4 can be used in research related to breast cancer.
(Pink: FAK ligand (HY-43760); Blue: VHL ligand (HY-125845); Black: linker (HY-W208616)).
For research use only. We do not sell to patients.
- Formula: C52H57F3N8O8S
- Molecular Weight:1011.12
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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
Description
IC50 & Target
[1]|
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | DC50 |
3.6 nM
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Dose-dependent FAK degradation in human breast cancer MDA-MB-231 cells measured via Western blot after 24 h treatment.
Dose-dependent FAK degradation in human breast cancer MDA-MB-231 cells measured via Western blot after 24 h treatment.
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41005113 |
| MDA-MB-231 | IC50 |
2.3 μM
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Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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41005113 |
In Vitro
PROTAC FAK degrader 4 (Compound 9C) (10-1000 nM; 8-32 h) potently and dose-dependently degrades FAK in MDA-MB-231 cells, with a DC50 of 3.6 nM; in addition, this compound induces persistent degradation of FAK, which reaches the maximum effect at 16 h and lasts until 32 h[1].
PROTAC FAK degrader 4 (10-300 nM; 24 h) induces dose-dependent degradation of FAK in breast cancer MCF-7 cells[1].
PROTAC FAK degrader 4 (72 h) potently inhibits the proliferation of MDA-MB-231 cells, with an IC50 value of 2.3 μM[1].
PROTAC FAK degrader 4 (2 μM; 72 h) acts synergistically with Cisplatin (HY-17394) to enhance the chemosensitivity of MDA-MB-231 cells; when used in combination at a concentration of 2 μM, it reduces the IC50 of cisplatin from 2.8 μM to 0.62 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human breast cancer MDA-MB-231 cells
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Concentration:10-100 nM (24 h); 0.3-1000 nM (24 h); 100 nM (time-course)
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Incubation Time:24 h (dose-response); 8-32 h (100 nM)
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Result:Induced FAK degradation with ratios exceeding 90% at 10 and 100 nM for 24 h.
Demonstrated dose-dependent FAK degradation with a DC50 of 3.6 nM and D_max of 95% after 24 h treatment.
Induced substantial FAK degradation as early as 8 h, with maximal degradation at 16 h maintained up to 32 h.
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Cell Line:human breast cancer MDA-MB-231 cells
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Concentration:serial dilutions
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Incubation Time:72 h
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Result:Potently inhibited MDA-MB-231 cell proliferation with an IC50 value of 2.3 μM.
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Cell Line:human breast cancer MDA-MB-231 cells
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Concentration:2 μM (PROTAC FAK degrader 4); serial dilutions (cisplatin)
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Incubation Time:72 h
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Result:Demonstrated a synergistic effect with cisplatin, with an HSA synergy score of 18.71.
Reduced the IC50 of cisplatin from 2.8 μM to 0.62 μM when co-treated at 2 μM.
Chemical Information
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Molecular Weight 1011.12
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Formula C52H57F3N8O8S
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SMILES
O=C([C@H]1N(C([C@@H](NC(C[C@H]2CC[C@H](NC(C3=CC=C(NC4=NC=C(C(F)(F)F)C(OC5=CC=CC(CC6)=C5C6=O)=N4)C(OC)=C3)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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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 4 Related Classifications
HY-178467 Related Classifications
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