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

PROTAC FGFR2 degrader 1 (compound N5) 是一种有效靶向 FGFR2 的 PROTAC，DC50 为 6.46 nM，IC50 为 0.08 nM。 PROTAC FGFR2 degrader 1 具有抗增殖活性和高度选择性，通过降低 FGFR2 下游蛋白 p-ERK 和 p-PLCγ 的激活，诱导 KATOIII 和 SNU16 周期阻滞于 G0/G1 期，抑制细胞凋亡 (Apoptosis)。 PROTAC FGFR2 degrader 1 在 0.17 nM 浓度下对胃癌细胞的抑制率保持在50%以上。 PROTAC FGFR2 degrader 1 有效抑制了小鼠模型中 SNU16 异种移植肿瘤的生长 (Srtucture Note: Pink，FGFR2 激活剂：HY-18708; Blue，E3 连接酶配体：HY-10984; Black，linker：HY-163989; E3连接酶配体 + 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 相关抗体

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

PROTAC FGFR2 degrader 1 (0-1000 nM; 72 h) 对 KATO III 和 SNU16 的 IC50 均小于 0.17 nM[1]。
PROTAC FGFR2 degrader 1 (500 nM; 12 h; WB) 诱导 KATO III 中 FGFR2 降解，对 FGFR2 具有高度选择性，且是 UPS 依赖性的[1]。
PROTAC FGFR2 degrader 1 (500，1000 nM; 24 h) 诱导 KATO III 和 SNU16 细胞在 G0/G1 期的细胞周期阻滞。

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

PROTAC FGFR2 degrader 1 相关抗体:

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.
体内研究
(In Vivo)

PROTAC FGFR2 degrader 1 (10 mg/kg, 20 mg/kg; Intraperitoneal injection) 在皮下异种移植 SNU16 小鼠模型中抑制胃癌细胞生长，降低肿瘤重量[1]。
PROTAC FGFR2 degrader 1在SD大鼠体内的药动学特征[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

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.
分子量

858.98

Formula

C46H54N10O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC FGFR2 degrader 1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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