2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FAK
  4. 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.

PROTAC FAK degrader 5

PROTAC FAK degrader 5 Chemical Structure

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PROTAC FAK degrader 5 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: FAK ligand (HY-183769); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

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.

PROTAC FAK degrader 5 Related Antibodies

Western Blot Analysis[1]

Cell Line: human colorectal cancer HCT116 cells
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)
Incubation Time: 0.5, 1, 2, 4, 6, 12, 24, 48, 72 h (5 μM concentration); 24 h (0.020-20 μM concentrations)
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.

Cell Proliferation Assay[1]

Cell Line: human colorectal cancer HCT116 cells
Concentration: 0.25, 0.5, 1, 2 μM
Incubation Time: 10 days
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.
Parmacokinetics
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
In Vivo

PROTAC FAK degrader 5 (compound 16g) (2 mg/kg; i.v.; single dose) demonstrates moderate clearance, extensive tissue distribution, and relatively rapid elimination from systemic circulation following a single 2 mg/kg intravenous dose in male Sprague-Dawley rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

826.78

Formula

C40H37F3N10O7
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC FAK degrader 5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC FAK degrader 5PROTAC FAK degrader5PROTAC FAK degrader-5PROTACsFAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasefocal adhesion kinaseHCT116 colorectal cancer cellhuman umbilical vein endothelial HUVEC cellcolorectal cancerendothelial cellscancer cellsFAK proteinL02 cellsmale Sprague-Dawley ratsInhibitorinhibitorinhibit

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