2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR Apoptosis Caspase
  4. FGFR3-IN-12

FGFR3-IN-12 是一种选择性成纤维细胞生长因子受体 3 (FGFR3) 抑制剂，其 IC50 为 6.8 nM。FGFR3-IN-12 对 FGFR3V555M 的 IC50 为 19.2 nM，对 TNK1 (三十八负激酶 1) 的 IC50 为 16.9 nM。FGFR3-IN-12 可抑制癌细胞增殖并诱导 caspase 介导的细胞凋亡 (apoptosis)。FGFR3-IN-12 在膀胱癌异种移植小鼠模型中展现出抗肿瘤活性。FGFR3-IN-12 可用于癌症相关研究，例如膀胱癌。

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FGFR3-IN-12

FGFR3-IN-12 Chemical Structure

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FGFR3-IN-12 相关抗体

Top Publications Citing Use of Products

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC50 of 6.8 nM. FGFR3-IN-12 shows an IC50 of 19.2 nM against FGFR3V555M and an IC50 of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer[1].

IC50 & Target[1]

FGFR3

6.8 nM (IC50)

FGFR2

35.7 nM (IC50)

FGFR1

296.2 nM (IC50)

FGFR4

414.5 nM (IC50)

体外研究
(In Vitro)

FGFR3-IN-12 (Compound 10s) 可强效抑制野生型 FGFR3，其 IC50 为 6.8 nM，且对野生型 FGFR1、FGFR2 和 FGFR4 展现出 5-60 倍的选择性[1]。
FGFR3-IN-12 (30 min) 对 FGFR3V555M 突变体具有抑制作用，其 IC50 为 19.2 nM[1]。
FGFR3-IN-12 (5 days) 可强效抑制由 FGFR3 驱动的 RT112/84 膀胱癌细胞的增殖，其 IC50 为 9.2 nM，且对 FGFR1 扩增、FGFR2 突变及 FGFR4 突变的癌细胞系具有 3.2 至 48.6 倍的选择性[1]。
FGFR3-IN-12 (0.5 μM) 表现出极佳的激酶组选择性 (S1 = 0.006，S10 = 0.012)，并以 16.9 nM 的 IC50 强效抑制 TNK1[1]。
FGFR3-IN-12 (1 h) 可与重组 FGFR3 共价结合，在 1:2 (FGFR3:FGFR3-IN-12) 摩尔比下孵育 1 小时后形成加合物[1]。
FGFR3-IN-12 (2 h) 会在 FGFR3 与 FGFR3-IN-12 摩尔比为 1:5 的条件下孵育 2 h 后，对 FGFR3 激酶结构域中的 Cys482 残基进行共价修饰[1]。
FGFR3-IN-12 (6.25-100 nM; 6-48 h) 可浓度依赖性地抑制 FGFR3 信号通路并诱导 RT112/84 膀胱癌细胞发生凋亡，同时可抑制工程化 Ba/F3 细胞中的 FGFR3V555M 信号通路[1]。
FGFR3-IN-12 (20-80 nM; 96 h) 可浓度依赖性地激活 RT112/84 膀胱癌细胞中的 Caspase-3/7[1]。

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

FGFR3-IN-12 相关抗体:

Western Blot Analysis[1]

Cell Line: RT112/84 bladder carcinoma cells, Ba/F3-FGFR3V555M engineered cells
Concentration: 6.25-100 nM (RT112/84 cells); 5-80 nM (Ba/F3-FGFR3V555M cells)
Incubation Time: 48 h (RT112/84 cells); 6 h (Ba/F3-FGFR3V555M cells)
Result: Caused a concentration-dependent reduction in phosphorylated FGFR3, phosphorylated ERK, and phosphorylated AKT in RT112/84 cells, with no change in total FGFR3, ERK, or AKT levels.
Induced concentration-dependent cleavage of PARP and activation of Caspase-7 in RT112/84 cells.
Caused a concentration-dependent reduction in phosphorylated FGFR3, phosphorylated MAPK, and phosphorylated AKT in Ba/F3-FGFR3V555M cells, with no change in total FGFR3, MAPK, or AKT levels.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUClast AUC0-inf F CL
Rat[1] 2.0 mg/kg i.v. 0.47 h 0.083 h 656 ng/mL 249 ng·h/mL 251 ng·h/mL / 133.4 mL/min/kg
Rat[1] 10.0 mg/kg p.o. 0.59 h 0.25 h 69.3 ng/mL 46.6 ng·h/mL 47.07 ng·h/mL 3.74 % /
体内研究
(In Vivo)

FGFR3-IN-12 (Compound 10s) (20-40 mg/kg；腹腔注射；每天一次；15 天) 在裸鼠的 RT112/84 膀胱癌异种移植模型中表现出剂量依赖性的抗肿瘤功效，在 40 mg/kg 剂量下实现了 77.1% 的最大肿瘤生长抑制率，且未观察到显著毒性[1]。

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

Animal Model: BALB/C nude with RT112/84 bladder cancer xenografts (female, 4 weeks old)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: I.p.; daily for 15 days
Result: Achieved 43.5% tumor growth inhibition at 20 mg/kg.
Achieved 77.1% tumor growth inhibition at 40 mg/kg.
Reduced tumor weight significantly relative to controls at both doses, with greater efficacy at 40 mg/kg.
Caused no significant body weight loss (>10%) or overt toxicity during treatment.
Suppressed Ki-67 staining in a dose-dependent manner, indicating reduced tumor cell proliferation.
分子量

486.57

Formula

C26H30N8O2
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-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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-12FGFRApoptosisCaspaseFibroblast growth factor receptorbladder cancer cellsTNK1FGFR4bladder cancerFGFR2FGFR1RT112/84 bladder carcinoma cellsFGFR3 V555MFGFR3bladder cancer xenograft modelsInhibitorinhibitorinhibit

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