2. PROTAC Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs FGFR ERK
  4. DGY-09-192

DGY-09-192 是一种 PROTAC FGFR1/2 降解剂 (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM)。DGY-09-192 优先降解野生型 FGFR1/2 以及多种 FGFR2 融合蛋白 (包括 FGFR2-PHGDH 和 FGFR2-OPTN)。DGY-09-192 在体外和体内抑制下游 FGFR 信号通路 (减少 FRS2 Y196 和 ERK1/2 T202/Y204 的磷酸化)。DGY-09-192 可用于研究 FGFR 驱动的癌症。(粉色：FGFR1/2 配体：(HY-160013)，蓝色：VHL 配体 (HY-112078)，黑色：连接子 (HY-W020017))。

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DGY-09-192

DGY-09-192 Chemical Structure

CAS No. : 2504949-52-2

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DGY-09-192 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017))[1].

IC50 & Target[1]

VHL

 

FGFR1

4.35 nM (DC50)

FGFR2

70 nM (DC50)

体外研究
(In Vitro)

DGY-09-192 (0.01-10 μM, 6 h) 在 KATO III 细胞中诱导 FGFR2 的剂量依赖性降解，DC50 为 70 nM，Dmax 为 74%[1]。
DGY-09-192 (0.1-1 μM, 24 h) 在 CCLP-1-FP 细胞(异位表达 FGFR2-PHGDH 融合蛋白) 和 ICC13-7 细胞 (内源性表达 FGFR2-OPTN 融合蛋白) 中导致 FGFR2-PHGDH 融合蛋白和 FGFR2-OPTN 融合蛋白的剂量依赖性降解[1]。
DGY-09-192 (0.1-10 μM, 16 h) 在 CCLP1 细胞 (过表达 FGFR1) 中有效降解 FGFR1，DC50 为 4.35 nM，Dmax 为 85%[1]。
DGY-09-192 (0.0001-100000 nM, 72 h) 对 KATO III 细胞 (IC50 = 1 nM)、CCLP1 细胞 (IC50 = 17 nM)、ICC13-7 细胞 (IC50 = 40 nM) 和 CCLP-FP 细胞 (IC50 = 8 nM) 显示出抗增殖活性[1]。
DGY-09-192 (50 nM, 4-8 h) 在 CCLP1-FP 细胞中持续抑制下游 FGFR2 信号通路[1]。

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

DGY-09-192 相关抗体:

Western Blot Analysis[1]

Cell Line: CCLP1-FP cells
Concentration: 50 nM
Incubation Time: 4, 8 h
Result: Suppressed the phosphorylation of FRS2 at Y196 and ERK1/2 at T202/Y204.
体内研究
(In Vivo)

DGY-09-192 (20-40 mg/kg，腹腔注射，每日一次，持续 6 天) 在 CCLP1-FGFR2-PHGDH 异种移植肿瘤模型中诱导 FGFR2-PHGDH 融合蛋白水平以及下游标志物 FRS2 (Y196) 和 ERK1/2 (T202/Y204) 磷酸化的减少[1]。

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

Animal Model: CCLP1-FGFR2-PHGDH xenograft tumor model: CCLP1 cells with ectopic expression of FGFR2-PHGDH fusion protein were used to establish xenograft tumors[1]
Dosage: 20 mg/kg and 40 mg/kg
Administration: i.p., once daily, 6 days
Result: Induced dose-dependent reduction in FGFR2-PHGDH fusion protein levels in tumor tissues.
Caused dose-dependent decrease in phosphorylation of downstream signaling markers FRS2 (Y196) and ERK1/2 (T202/Y204) in tumor tissues.
分子量

1017.03

Formula

C49H59Cl2N11O7S
CAS 号
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

DGY-09-192 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

DGY-09-1922504949-52-2PROTACsFGFRERKFibroblast growth factor receptorExtracellular signal regulated kinasesFGFR1/2PROTACICC13-7 cellsCCLP-1-FP cellsKATO III cellsInhibitorinhibitorinhibit

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产品名称：
DGY-09-192
目录号：
HY-165298
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