2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. PROTAC FGFR3 Degrader-1

PROTAC FGFR3 Degrader-1 是成纤维细胞生长因子受体 3 (FGFR3)，可通过泛素-蛋白酶体通路促进 FGFR3 降解，并抑制下游 FGFR3/PI3K/AKT 信号通路。PROTAC FGFR3 Degrader-1 可用于肝细胞癌的相关研究。
(粉色: FGFR 配体 (HY-181152)；蓝色: Ligands for E3 Ligase 配体 (HY-14658)；黑色: 连接子)。

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PROTAC FGFR3 Degrader-1

PROTAC FGFR3 Degrader-1 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

PROTAC FGFR3 Degrader-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3), promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma[1]. (Pink: FGFR ligand (HY-181152); Blue: Ligands for E3 Ligase ligand (HY-14658); Black: linker).

体外研究
(In Vitro)

PROTAC FGFR3 Degrader-1 (48 h) 可强效抑制 Huh-7、HepG2 和 MHCC97-H 肝癌细胞的增殖，其 IC50 值分别为 0.56 μM、1.44 μM 和 1.87 μM[1]。
PROTAC FGFR3 Degrader-1 (0.125-1 μM; 24 h) 可通过蛋白酶体通路以剂量依赖方式诱导 Huh-7 细胞中 FGFR3 蛋白降解，且该降解作用会被 B10 或泊马度胺 (pomalidomide) 联合处理所抑制[1]。
PROTAC FGFR3 Degrader-1 (0.25-1 μM; 6-24 h) 可在 Huh-7 细胞中以时间和剂量依赖的方式下调 FGFR3 表达，并抑制 FGFR3/PI3K/AKT 信号通路的活性[1]。
PROTAC FGFR3 Degrader-1 (40 μM) 可在 Huh-7 细胞中与 FGFR3 稳定结合，这一点已通过细胞热位移实验中它保护 FGFR3 免于热变性的能力得到证实[1]。
PROTAC FGFR3 Degrader-1 (10-40 μM) 可在 Huh-7 细胞裂解液中与 FGFR3 稳定结合，这一点在药物亲和力响应靶标稳定性实验中得到证实：该化合物可呈剂量依赖性地保护 FGFR3 免受链霉蛋白酶的酶解[1]。
PROTAC FGFR3 Degrader-1 可通过分子对接预测，以-7.5 kcal/mol 的结合能与 FGFR3 稳定结合[1]。

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

PROTAC FGFR3 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 0.125-1 μM (degradation efficiency assessment); 1 μM (24 h treatment alone); 10 μM MG132 (co-treatment); 1 μM B10 (co-treatment); 10 μM pomalidomide (co-treatment)
Incubation Time: 24 h (1 μM treatment; co-treatments)
Result: Promoted dose-dependent degradation of FGFR3 protein, with significant degradation observed at 0.5 μM and 1 μM. Had its induced FGFR3 degradation rescued by co-treatment with MG132, had its induced FGFR3 degradation inhibited by co-treatment with its precursor B10, and had its induced FGFR3 degradation inhibited by co-treatment with the CRBN E3 ligase ligand pomalidomide.

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 0.25-1 μM (dose-dependent assessment); 1 μM (time-dependent assessment)
Incubation Time: 6 h, 12 h, 24 h (1 μM treatment)
Result: Downregulated FGFR3 expression and inhibited PI3K/AKT pathway activity in a time- and dose-dependent manner. Had its induced suppression of PI3K/AKT pathway activity significantly reversed by activation of FGFR3.
分子量

844.04

Formula

C46H53N9O5S
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 FGFR3 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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 FGFR3 Degrader-1FGFRFibroblast growth factor receptorFGFR3/PI3K/AKT signaling pathwayHuh-7HepG2PI3Kfibroblast growth factor receptor 3ubiquitin-proteasome pathwayMHCC97-Hproteasome pathwayFGFR3hepatocellular carcinomaInhibitorinhibitorinhibit

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目录号：
HY-181153
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