PROTAC FGFR2 degrader 1

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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 (Structure 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

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.)
t_1/2 (h)	4.65±4.14	t_1/2 (h)	7.59±0.365
T_max (h)	/	T_max (h)	0.25±0.177
C_max (ng/mL)	/	C_max (ng/mL)	302±33.7
MRT_inf (h)	2.27±1.44	MRT_inf (h)	6.53±0.0721
CL (mL/min/kg)	59.3±8.35	CL/F (mL/min/kg)	78.2±1.62
V_ss (L/kg)	7.58±3.80	V_Z/F (L/kg)	51.4±2.40
AUC_0-t (h*ng/mL)	544±74.2	AUC_0-t (h*ng/mL)	991±20.7
AUC_0-inf (h*ng/mL)	570±83.3	AUC_0-inf (h*ng/mL)	1066±21.9
AUC_0-t/ AUC_0-inf	0.956±0.0232	AUC_0-t/ AUC_0-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

Handling Instructions (2659 KB)

References

[1]. Zhanzhan Feng, et al. Synthesis and identification of a selective FGFR2 degrader with potent [Content Brief]