2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs FGFR Apoptosis
  4. PROTAC FGFR2 degrader 1

PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Srtucture Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .

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PROTAC FGFR2 degrader 1 Chemical Structure

PROTAC FGFR2 degrader 1 Chemical Structure

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PROTAC FGFR2 degrader 1 Related Antibodies

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Description

PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Srtucture Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) [1].

IC50 & Target

FGFR2

 

In Vitro

PROTAC FGFR2 degrader 1 (0-1000 nM, 72 h) IC50 is less than 0.17 nM for both Kato III and SNU16[1].< br/> PROTAC FGFR2 degrader 1 (500 nM; 12 h; WB) induces FGFR2 degradation in Kato III, which is highly selective for FGFR2 and UPS-dependent[1].< br/> PROTAC FGFR2 degrader 1 (500, 1000 nM; 24 h) induces cell cycle arrest of Kato III and SNU16 cells in G0/G1 phase[1].

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

PROTAC FGFR2 degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: KATO III, SNU16
Concentration: 0, 0.1, 1, 10, 100, 500, 1000 nM
Incubation Time: 0, 1, 6, 12, 24, 36 h
Result: Degraded FGFR2 in Kato III cells with timedependent. Induced FGFR2 degradation in SNU16 cells in vivo in a mouse model. Decreased CDK2, CDK 4, Cyclin D1 and Cyclin E.

Western Blot Analysis[1]

Cell Line: KATO III, SNU16
Concentration: 500 nM, 12 h; Pomalidomide (10 μM), Erdafitinib (10 μM), MG132 (5 μM) for 6 h; 50, 100, 500 nM for 24 h
Incubation Time: 12 h; 24 h
Result: Degraded FGFR2 via the UPS pathway, and degradation of FGFR2 was dependent on the formation of the FGFR2-N5-E3 ligase complex and subsequent proteasomal degradation. Showed that phosphorylation of p-AKT was decreased in both SNU16 and Kato III cells, inhibited the activation of p-ERK and p-PLC γ effectively.

Real Time qPCR[1]

Cell Line: KATO III
Concentration: 500 nM
Incubation Time: 12 h
Result: Degraded FGFR2 in KATOIII with high selectivity.

Cell Cycle Analysis[1]

Cell Line: KATO III, SNU16
Concentration: 500, 1000 nM
Incubation Time: 24 h
Result: Showed that the percentage of KATO III cells in the G0/G1 phase increased from 47.7% to 67.1% in the 1000 nM of PROTAC FGFR2 degrader 1, the number of SNU16 cells increased from 45.9% to 67.5%.

Apoptosis Analysis[1]

Cell Line: KATO III, SNU16
Concentration: 1000 nM
Incubation Time: 24 h
Result: Showed that the apoptosis rate of KATO III cells increased from 10.9% in the DMSO group to 30.5%, upregulation of cleaved caspase 3 was observed.
In Vivo

PROTAC FGFR2 degrader 1 (10 mg/kg, 20 mg/kg; Intraperitoneal injection) inhibits gastric cancer growth in the SNU16 subcutaneous xenograft tumor model in vivo[1].
Pharmacokinetic profiles of PROTAC FGFR2 degrader 1 in SD rats.[1]

Parameters PROTAC FGFR2 degrader 1 2mg/kg(i.v.) Parameters PROTAC FGFR2 degrader 1 2mg/kg(i.p.)
t1/2 (h) 4.65±4.14 t1/2 (h) 7.59±0.365
Tmax (h) / Tmax (h) 0.25±0.177
Cmax (ng/mL) / Cmax (ng/mL) 302±33.7
MRTinf (h) 2.27±1.44 MRTinf (h) 6.53±0.0721
CL (mL/min/kg) 59.3±8.35 CL/F (mL/min/kg) 78.2±1.62
Vss (L/kg) 7.58±3.80 VZ/F (L/kg) 51.4±2.40
AUC0-t (h*ng/mL) 544±74.2 AUC0-t (h*ng/mL) 991±20.7
AUC0-inf (h*ng/mL) 570±83.3 AUC0-inf (h*ng/mL) 1066±21.9
AUC0-t/ AUC0-inf 0.956±0.0232 AUC0-t/ AUC0-inf 0.930±0.00429
F / F (%) 74.8±1.53

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

Animal Model: SD rats[1]
Dosage: 2, 5 mg/kg
Administration: Intravenous injection (i.v.); Intraperitoneal injection (i.p.)
Result: Absorbed rapidly in vivo, reached its maximum concentration at 0.25 h by 5 mg/kg, and then slowly cleared from the body, with a half-life of 7.59 h.
Animal Model: A mouse model of subcutaneous xenograft of SNU16 tumor[1]
Dosage: 10, 20 mg/kg
Administration: Intraperitoneal injection(i.p.); once daily; 25 days
Result: Showed the stronger anti-tumor effect, greater tumor growth inhibition and a significant reduction in tumor weight.
Molecular Weight

858.98

Formula

C46H54N10O7
SMILES

COC1=CC(OC)=CC(N(C2=CC=C3N=CC(C4=CN(N=C4)CCCCCCC(NCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=NC3=C2)CCNC(C)C)=C1
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 FGFR2 degrader 1 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 FGFR2 degrader 1PROTACsFGFRApoptosisFibroblast growth factor receptorPROTACGastric cancer cellsAnti-proliferationInhibitorinhibitorinhibit

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