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PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.
Pack Size | Price | Availability | Quantity |
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10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model. |
In vitro | PROTAC FGFR2 degrader 1 exhibits potent inhibitory activity in KATO III and SNU16 cells, with IC50 values below 0.17 nM (0-1000 nM; 72 h). Additionally, this compound (500 nM; 12 h; WB) selectively induces degradation of FGFR2 in KATO III, operating via the UPS pathway. Also, when administered at concentrations of 500 and 1000 nM over 24 hours, PROTAC FGFR2 degrader 1 induces cell cycle arrest at the G0/G1 phase in both KATO III and SNU16 cells. |
In vivo | PROTAC FGFR2 degrader 1, when administered at doses of 10 mg/kg and 20 mg/kg via intraperitoneal injection, suppresses the growth of gastric cancer cells and reduces tumor weight in a subcutaneous xenograft SNU16 mouse model. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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