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.
- Formula: C46H45F4N9O8
- Molecular Weight:927.90
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
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Cell Line:MDA-MB-231 cells
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Concentration:0.01; 0.03; 0.1; 0.3; 1; 3; 10 μM
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Incubation Time:6; 12; 48; 72 h
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Result:Reduced FAK levels in a dose-dependent manner.
Reduced FAK levels in a time-dependent manner at 1 μM.
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Cell Line:4T1, MDA-MB-231
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Concentration:1 μM
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Incubation Time:24; 48; 72 h
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Result:Inhibited the migration rate in both 4T1 and MDA-MB-231 cells.
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Cell Line:4T1, MDA-MB-231
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Concentration:1 μM
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Incubation Time:48 h
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Result:Suppressed cell invasion more significantly
than F1 in both 4T1 and MDA-MB-231 cells
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 5-6 weeks old, 16-18 g) subcutaneously implanted with HCT8/T cells[1]
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Dosage:15 mg/kg
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Administration:i.p.; daily; 14 days
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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.
Chemical Information
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Molecular Weight 927.90
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Formula C46H45F4N9O8
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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
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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 2 Related Classifications
HY-163709 Related Classifications
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