2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-13

FGFR-IN-13 (compound III-30) 通过抑制关键蛋白的表达调节内源性 FGFR1(IC50=0.20±0.02 nM) 和 FGFR4(IC50=0.40±0.03 nM) 介导的信号通路。FGFR-IN-13 能够抑制 total-PARP 和 Bcl-2 蛋白的表达，促进 Cleaved-PARP 和 Bax 蛋白的表达，且呈剂量依赖性。FGFR-IN-13 具有显著的抗肿瘤活性且具有口服活性。

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FGFR-IN-13

FGFR-IN-13 Chemical Structure

CAS No. : 2962941-25-7

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FGFR-IN-13 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

FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HUVEC IC50
82.14 μM
Compound: III-30
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38643670]
HepG2 IC50
7.93 μM
Compound: III-30
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38643670]
MDA-MB-231 IC50
1.89 μM
Compound: III-30
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38643670]
MDA-MB-435 IC50
9.17 μM
Compound: III-30
Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38643670]
体外研究
(In Vitro)

FGFR-IN-13 (10 μM, 9 h) 可以和 FGFR 蛋白实现共价不可逆结合，其抑制 p-FGFR 蛋白表达的能力可以达到 AZD4547(HY-13330) 和 TAS-120(HY-100818) 的水平在 MDA-MB-231 细胞系中[1]。
FGFR-IN-13 (2.5, 5, 10 μM, 24 h) 能呈剂量依赖性诱导细胞凋亡， 在相同浓度 (5 μM) 下诱导凋亡能力优于AZD4547 (45.4% 和 37.3%)， 可能具有与 AZD4547 相似的作用机制，但 MDAMB-231 细胞对 III-30 更为敏感[1]。 FGFR-IN-13 (1.25, 2.5, 5 μM, 12 h) 在不产生明显细胞毒性的剂量下，能有效抑制MDA-MB-231细胞的迁移，且呈剂量依赖性[1]。 FGFR-IN-13 (2.5, 5, 10 μM, 12 h) 能够通过产生过量的ROS和降低MMP来诱导细胞凋亡[1]。

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

FGFR-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 9 h
Result: Inhibited the autophosphorylation of FGFR protein for a long period of time, and the expression level of p-FGFR protein in cancer cells is still suppressed even after 8 h of discontinuation.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, and the percentage of induced apoptosis reached 56.8 % at 10 μM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB- 435, MDA-MB-231, KYSE-150, HepG2 and HUVEC cells
Concentration:
Incubation Time: 72 h
Result: Showed better inhibitory effect on KYSE-150 cells (IC50 = 1.93 μM) compared with 2 positive controls.
体内研究
(In Vivo)

FGFR-IN-13 (10 和 30 mg/kg， 每天口服一次持续 21 天) 抑制肿瘤生长呈剂量依赖性，且具有良好的安全性，在安全剂量下可有效抑制肿瘤生长在 MDA-MB-231 异种移植瘤小鼠模型[1]。

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

Animal Model: MDA-MB-231 xenograft tumor mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Did not cause significant weight loss.
Achieved tumor growth inhibition (TGI) of 64.21% at high doses (30 mg/kg).
Achieved tumor growth inhibition (TGI) of 40.22% at low doses (10 mg/kg).
分子量

415.44

Formula

C23H21N5O3
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

FGFR-IN-13 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:

FGFR-IN-132962941-25-7FGFRFibroblast growth factor receptorFGFR inhibitorIrreversible covalent inhibitorAnti-tumor activityMDA-MB-231 xenograft tumor mouse modelInhibitorinhibitorinhibit

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