| Bioactivity | PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))[1] |
| Formula | C46H45F4N9O8 |
| Molar Mass | 927.90 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xu MS, et al., A novel FAK-degrading PROTAC molecule exhibited both anti-tumor activities and efficient MDR reversal effects. Acta Pharmacol Sin. 2024 Jun 6. |
PROTAC FAK degrader 2
CAS: F: C46H45F4N9O8 W: 927.90
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM
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