2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR3-IN-11

FGFR3-IN-11 (compound B11) 是一种成纤维细胞生长因子受体 3 (FGFR3) 抑制剂，其 Ka 值为 4.8 μM。FGFR3-IN-11 可诱导癌细胞凋亡、抑制集落形成，并导致癌细胞出现剂量依赖性 G0/G1 期细胞周期阻滞。FGFR3-IN-11 对癌细胞具有抗癌活性，而对正常肝细胞的毒性极低，且在异种移植小鼠模型中可抑制肿瘤生长。FGFR3-IN-11 可用于肝细胞癌的研究。

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FGFR3-IN-11

FGFR3-IN-11 Chemical Structure

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FGFR3-IN-11 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

FGFR3-IN-11(compound B11) is a Fibroblast growth factor receptor 3 (FGFR3) inhibitor with a Ka value of 4.8 μM. FGFR3-IN-11 induces apoptosis, suppresses colony formation, and causes dose-dependent G0/G1 cell cycle arrest in cancer cells. FGFR3-IN-11 exerts anticancer activity against cancer cells with minimal toxicity toward normal hepatocytes and demonstrates tumor growth suppression in xenograft mouse models. FGFR3-IN-11 can be used for the research of hepatocellular carcinoma[1].

体外研究
(In Vitro)

FGFR3-IN-11 (B10) (48 h) 可强效抑制 Huh-7、HepG2 和 MHCC97-H 肝癌细胞系的增殖，其 IC50 值分别为 4.13、4.76 和 5.79 μM，且对 L02 正常肝细胞的毒性极低[1]。
FGFR3-IN-11 (B10) (1.25-5 μM；初始处理 48 小时，培养基更换周期 14 天) 以剂量依赖的方式抑制 Huh-7 肝癌细胞的集落形成[1]。
FGFR3-IN-11 (B10)(1.25-5 μM；作用 48 小时) 在 Huh-7 肝癌细胞中诱导呈剂量依赖性的 G0/G1 期阻滞[1]。
FGFR3-IN-11 (B10) (1.25-5 μM；作用 24 小时) 可在 Huh-7 肝癌细胞中诱导剂量依赖性细胞凋亡，同时 Bcl-2 和 Bax 蛋白水平出现相应变化[1]。
FGFR3-IN-11 (B10)(1.25-5 μM；作用 24 h) 可通过剂量依赖性降低总PI3K及磷酸化PI3K、AKT的水平，抑制 Huh-7 肝癌细胞中的 PI3K/AKT 信号通路[1]。
FGFR3-IN-11 (B10)(系列稀释浓度：40 μM、10-40 μM；DARTS 预孵育 1 小时) 可与 FGFR3 蛋白稳定结合，其 KD值为 4.8 μM，该结果已通过分子对接、SPR、CETSA 及 DARTS 实验验证[1]。

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

FGFR3-IN-11 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 48 h (initial treatment); 14 days (medium replacement)
Result: Significantly suppressed colony formation in Huh-7 cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 48 h
Result: Induced dose-dependent G0/G1 phase arrest in Huh-7 cells.

Apoptosis Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 24 h
Result: Induced dose-dependent apoptosis in Huh-7 cells. Downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic protein Bax in a dose-dependent manner (Western blot).

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 24 h
Result: Reduced the levels of total and phosphorylated PI3K and AKT in a dose-dependent manner.
体内研究
(In Vivo)

B10 (20-60 mg/kg；腹腔注射；每两日一次；持续 28 天) 在 Huh-7 异种移植模型中表现出强效的体内抗肿瘤活性，在 40 mg/kg 剂量下的肿瘤生长抑制率 (TGI) 达 64.18%，且具有良好的安全性特征[1]。

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

Animal Model: Balb/c nude mice (female, 4-6 weeks old, 18-19 g average weight)[1]
Dosage: 20, 40, 60 mg/kg; 40 mg/kg (TGI assessment)
Administration: i.p.; every other day; 28 days
Result: Achieved a tumor growth inhibition (TGI) rate of 64.18% at 40 mg/kg; Induced a dose-dependent decrease in phospho-FGFR3 (p-FGFR3) in tumor tissues; Caused a pronounced decrease in Ki-67-positive cells in tumors; Showed no significant weight loss compared to the control group.
分子量

449.65

Formula

C27H35N3OS
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

FGFR3-IN-11 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:

FGFR3-IN-11FGFRFibroblast growth factor receptorFGFR3/PI3K/AKT signaling pathwayhepatocytesxenograft mouse modelsFibroblast growth factor receptor 3Huh-7HepG2G0/G1 cell cycle arrestapoptosisMHCC97-Hhepatocellular carcinomaInhibitorinhibitorinhibit

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