2. PROTAC Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs FAK Akt ERK
  4. PROTAC FAK degrader 2

PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer.

For research use only. We do not sell to patients.

PROTAC FAK degrader 2

PROTAC FAK degrader 2 Chemical Structure

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PROTAC FAK degrader 2 Related Antibodies

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Description

PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer[1].

In Vitro

PROTAC FAK degrader 2 (compound F2) (0.01-10 μM; 6-72 h) targets and degrades FAK in MDA-MB-231 cells[1].
PROTAC FAK degrader 2 (72 h) inhibits cell growth of 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435 cells, with IC50 values of 0.73, 1.09, 5.84, and 3.05 μM, respectively[1].
PROTAC FAK degrader 2 (1 μM; 24-72 h) inhibits cell migration in 4T1 and MDA-MB-231 cells[1].
PROTAC FAK degrader 2 (1 μM; 48 h) inhibits cell invasion in 4T1 and MDA-MB-231 cells[1].

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

PROTAC FAK degrader 2 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.01; 0.03; 0.1; 0.3; 1; 3; 10 μM
Incubation Time: 6; 12; 48; 72 h
Result: Reduced FAK levels in a dose-dependent manner.
Reduced FAK levels in a time-dependent manner at 1 μM.

Cell Migration Assay [1]

Cell Line: 4T1, MDA-MB-231
Concentration: 1 μM
Incubation Time: 24; 48; 72 h
Result: Inhibited the migration rate in both 4T1 and MDA-MB-231 cells.

Cell Invasion Assay[1]

Cell Line: 4T1, MDA-MB-231
Concentration: 1 μM
Incubation Time: 48 h
Result: Suppressed cell invasion more significantly
than F1 in both 4T1 and MDA-MB-231 cells
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT
Mice[1] 1 mg/kg p.o. 3.36 h 2.00 h 272 ng/mL 2112 ng·h/mL 2129 ng·h/mL 5.18 h
In Vivo

PROTAC FAK degrader 2 (compound F2) (15 mg/kg; i.p.; daily; 14 days) exhibits anti-tumor activity and potent Paclitaxel resistance reversal activity in Paclitaxel (HY-B0015)-resistant HCT8/T mouse xenograft tumors[1].

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

Animal Model: BALB/c nude mice (female, 5-6 weeks old, 16-18 g) subcutaneously implanted with HCT8/T cells[1]
Dosage: 15 mg/kg
Administration: i.p.; daily; 14 days
Result: Produced a tumor growth inhibition (TGI) rate of 26.89%, with mean tumor volume increasing from 114.1 mm3 to 779.3 mm3 over 14 days.
Increased the TGI rate to 51.24% when combined with Paclitaxel (HY-B0015), with mean tumor volume increasing from 114.6 mm3 to 519.5 mm3 over 14 days.
Molecular Weight

927.90

Formula

C46H45F4N9O8
SMILES

COC1=CC(C(NC2CCN(CC2)CC3CCN(CC3)C4=CC5=C(C(N(C5=O)C6CCC(NC6=O)=O)=O)C=C4)=O)=C(C=C1NC7=NC(OC8=CC=CC9=C8C(N(C9)C)=O)=C(C=N7)C(F)(F)F)F
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 2 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 2PROTAC FAK degrader2PROTAC FAK degrader-2PROTACsFAKAktERKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePKBProtein kinase BExtracellular signal regulated kinasesepithelial-mesenchymal transitionHCT8/TAKTproteasomeSlugN-cadherinCRBN E3 ubiquitin ligaseP-glycoproteinInhibitorinhibitorinhibit

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